Bibliographies thématiques / Biologically potent molecules

Littérature scientifique sur le sujet « Biologically potent molecules »

Auteur : Grafiati
Publié le 18 mai 2024

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Articles de revues sur le sujet "Biologically potent molecules"

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Fotopoulos, Ioannis, et Dimitra Hadjipavlou-Litina. « Hybrids of Coumarin Derivatives as Potent and Multifunctional Bioactive Agents : A Review ». Medicinal Chemistry 16, no 3 (17 avril 2020) : 272–306. http://dx.doi.org/10.2174/1573406415666190416121448.

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Background: Coumarins exhibit a plethora of biological activities, e.g. antiinflammatory and anti-tumor. Molecular hybridization technique has been implemented in the design of novel coumarin hybrids with several bioactive groups in order to obtain molecules with better pharmacological activity and improved pharmacokinetic profile. Objective: Therefore, we tried to gather as many as possible biologically active coumarin hybrids referred in the literature till now, to delineate the structural characteristics in relation to the activities and to have a survey that might help the medicinal chemists to design new coumarin hybrids with drug-likeness and varied bioactivities. Results: The biological activities of the hybrids in most of the cases were found to be different from the biological activities presented by the parent coumarins. The results showed that the hybrid molecules are more potent compared to the standard drugs used in the evaluation experiments. Conclusion: Conjugation of coumarin with varied pharmacophore groups/druglike molecules responsible for different biological activities led to many novel hybrid molecules, with a multitarget behavior and improved pharmacokinetic properties.
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Thorat, Sagar S., et Ravindar Kontham. « Strategies for the synthesis of furo-pyranones and their application in the total synthesis of related natural products ». Organic Chemistry Frontiers 8, no 9 (2021) : 2110–62. http://dx.doi.org/10.1039/d0qo01421d.

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The furo-pyranone framework is widely present in the molecular structure of various biologically potent natural products and un-natural small molecules, and it represents a valuable target in synthetic organic chemistry and medicinal chemistry.
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Karageorgis, George, et Herbert Waldmann. « Guided by Evolution : Biology-Oriented Synthesis of Bioactive Compound Classes ». Synthesis 51, no 01 (11 octobre 2018) : 55–66. http://dx.doi.org/10.1055/s-0037-1610368.

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Biology-oriented-synthesis (BIOS), is a chemocentric approach to identifying structurally novel molecules as tools for chemical biology and medicinal chemistry research. The vast chemical space cannot be exhaustively covered by synthetic chemistry. Thus, methods which reveal biologically relevant portions of chemical space are of high value. Guided by structural conservation in the evolution of both proteins and natural products, BIOS classifies bioactive compound classes in a hierarchical manner based on molecular architecture and bioactivity. Biologically relevant scaffolds inspire and guide the synthesis of BIOS libraries, which calls for the development of suitable synthetic methodologies. These compound collections have enriched biological relevance, leading to the discovery of bioactive small molecules. These potent and selective modulators allow the study of complex biological pathways and may serve as starting points for drug discovery programs. Thus, BIOS can also be regarded as a hypothesis-generating tool, guiding the design and preparation of novel, bioactive molecular scaffolds. This review elaborates the principles of BIOS and highlights selected examples of their application, which have in turn created future opportunities for the expansion of BIOS and its combination with fragment-based compound discovery for the identification of biologically relevant small molecules with unprecedented molecular scaffolds.1 Introduction2 Structural Classification of Natural Products3 Implications and Opportunities for Biology-Oriented Synthesis4 Applications of Biology-Oriented Synthesis4.1 Chemical Structure and Bioactivity Guided Approaches4.2 Natural-Product-Derived Fragment-Based Approaches5 Conclusions and Outlook
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Wavhal, Kamalakar Kailash, et Deepak Manik Nagrik. « Synthesis of Biologically Potent α-Aminophosphonates Derivatives by Nano-Catalyst ». Oriental Journal Of Chemistry 38, no 5 (31 octobre 2022) : 1314–19. http://dx.doi.org/10.13005/ojc/380532.

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α-Aminophosphonate and their derivatives are biologically potent and have received considerable attention in a recent research scenario. The main reason is that they show triguing biological activity. α-Aminophosphonate derivatives are gaining a lot of importance in medicinal chemistry due to their application as enzyme inhibitors, herbicides, antibiotics, pharmaceutical agents and inhibitors of Excitatory Post-Synaptic Potential(EPSP) synthesis, and HIV Protease. It is also important in ati-cancer, anti-HIV, antithrombotic and antibacterial, antioxidant activity. Unfortunately, these compounds have certain limitation such as extraction, purification, of bioactive molecule and their minimum yields. For this reason, many scientists have been orienting their research towards the synthesis of molecules as a new tool to overcome this problems he prime focus of this work is the combination of three reactant derivative of benzaldehyde derivative of aniline, and diethyl phosphonate to form α-aminophosphonates derivatives by multicomponent reaction(KFR). The novel nano-catalyst i.e. polyanilinedoped with manganese (PAni-Mn) was prepared. The catalyst shows excellent catalytic activity, high yields, short reaction times, easy synthesis. The PAni was fully characterized by X-ray diffraction, TEM, SEM, and FT-IR technique.
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Naveen, Naveen, Ram Kumar Tittal, Pinki Yadav, Kashmiri Lal, Ghule Vikas D. et Ashwani Kumar. « Synthesis, molecular docking and DFT studies on biologically active 1,4-disubstituted-1,2,3-triazole-semicarbazone hybrid molecules ». New Journal of Chemistry 43, no 21 (2019) : 8052–58. http://dx.doi.org/10.1039/c9nj00473d.

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Biologically active semicarbazone-triazole hybrid molecules designed and synthesized from semicarbazone linked with a terminal alkyne and aromatic azidesviaCu(i)-catalyzed cycloaddition reaction. The synthesized compounds exhibited potent antibacterial activities against the tested bacterial strains. Computational results are in good agreement with thein vitroantimicrobial results.
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Gazieva, Galina A., et Konstantin Chegaev. « Special Issue “Development and Synthesis of Biologically Active Compounds” ». International Journal of Molecular Sciences 25, no 7 (4 avril 2024) : 4015. http://dx.doi.org/10.3390/ijms25074015.

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The intention of this Special Issue is to focus on new achievements in the design, preparation, and in vitro and in vivo biological evaluation of bioactive molecules that can result in the development of natural or artificial potent compounds looking for promising pharmaceuticals and agrochemicals [...]
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Mielcarek, Michal, et Mark Isalan. « Kinetin stimulates differentiation of C2C12 myoblasts ». PLOS ONE 16, no 10 (13 octobre 2021) : e0258419. http://dx.doi.org/10.1371/journal.pone.0258419.

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Kinetin or N6-furfuryladenine (K) belongs to a class of plant hormones called cytokinins, which are biologically active molecules modulating many aspects of plant growth and development. However, biological activities of cytokinins are not only limited to plants; their effects on animals have been widely reported in the literature. Here, we found that Kinetin is a potent small molecule that efficiently stimulates differentiation of C2C12 myoblasts into myotubes in vitro. The highest efficacy was achieved at 1μM and 10μM Kinetin concentrations, in both mitogen-poor and rich media. More importantly, Kinetin was able to strongly stimulate the MyoD-dependent conversion of fibroblasts into myotubes. Kinetin alone did not give rise to fibroblast conversion and required MyoD; this demonstrates that Kinetin augments the molecular repertoire of necessary key regulatory factors to facilitate MyoD-mediated myogenic differentiation. This novel Kinetin pro-myogenic function may be explained by its ability to alter intracellular calcium levels and by its potential to impact on Reactive Oxygen Species (ROS) signalling. Taken together, our findings unravel the effects of a new class of small molecules with potent pro-myogenic activities. This opens up new therapeutic avenues with potential for treating skeletal muscle diseases related to muscle aging and wasting.
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Islam, Rainul, Sumit Maji, Souparna Kabiraj, Umme Habib, Rohan Pal, Somenath Bhattacharya, Soumallya Chakraborty et Dr Arin Bhattacharjee. « Role of in silico Drug Design in Pharmaceutical Sciences ». International Journal for Research in Applied Science and Engineering Technology 10, no 5 (31 mai 2022) : 2358–67. http://dx.doi.org/10.22214/ijraset.2022.42836.

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Abstract: In silico drug design is the study to identify, develop, analyze, optimize drugs or biologically cum pharmaceutically active compounds by using computerized software programs as well web servers. In silico drug design is commonly known as computer aided drug design or CADD in short. This technique shows a vital role in preclinical drug design and development. CADD can improve the speed of drug design. It reduces time as well as total cost of the experiments. Potent cum suitable molecules are prepared after performing in silico drug design including CADD. Various applications like confirmation generation, homology modeling, multiple sequence alignment, molecular docking study, generation of Pharmacophores, virtual screening, de novo drug design, QSAR (Quantitative structure activity relationships) study, molecular modeling, in silico ADMET (Absorption, distribution, metabolism, excretion and toxicity) prediction of CADD has been implemented to design newer molecules. The current study focuses on different strategies cum approaches through computer aided drug designing applied to find potent, efficient and safe molecules in the field of drug discovery. Keywords: CADD, drug design, molecular docking, Pharmacophores, virtual screening, de novo drug design, QSAR, molecular modeling.
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Meyer, Claire E., Cora-Ann Schoenenberger, Juan Liu, Ioana Craciun et Cornelia G. Palivan. « DNA-tethered Polymersome Clusters as Nanotheranostic Platform ». CHIMIA International Journal for Chemistry 75, no 4 (28 avril 2021) : 296–99. http://dx.doi.org/10.2533/chimia.2021.296.

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Nanotheranostics combine the use of nanomaterials and biologically active compounds to achieve diagnosis and treatment at the same time. To date, severe limitations compromise the use of nanotheranostic systems as potent nanomaterials are often incompatible with potent biomolecules. Herein we emphasize how a novel type of polymersome clusters loaded with active molecules can be optimized to obtain an efficient nanotheranostic platform. Polymersomes loaded with enzymes and specific dyes, respectively and exposing complementary DNA strands at their external surface formed clusters by means of DNA hybridization. We describe factors at the molecular level and other conditions that need to be optimized at each step of the cluster formation to favor theranostic efficiency.
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Meena, Khem Raj, et Shamsher S. Kanwar. « Lipopeptides as the Antifungal and Antibacterial Agents : Applications in Food Safety and Therapeutics ». BioMed Research International 2015 (2015) : 1–9. http://dx.doi.org/10.1155/2015/473050.

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A lot of crops are destroyed by the phytopathogens such as fungi, bacteria, and yeast leading to economic losses to the farmers. Members of theBacillusgenus are considered as the factories for the production of biologically active molecules that are potential inhibitors of growth of phytopathogens. Plant diseases constitute an emerging threat to global food security. Many of the currently available antimicrobial agents for agriculture are highly toxic and nonbiodegradable and thus cause extended environmental pollution. Moreover, an increasing number of phytopathogens have developed resistance to antimicrobial agents. The lipopeptides have been tried as potent versatile weapons to deal with a variety of phytopathogens. All the three families ofBacilluslipopeptides, namely, Surfactins, Iturins and Fengycins, have been explored for their antagonistic activities towards a wide range of phytopathogens including bacteria, fungi, and oomycetes. Iturin and Fengycin have antifungal activities, while Surfactin has broad range of potent antibacterial activities and this has also been used as larvicidal agent. Interestingly, lipopeptides being the molecules of biological origin are environmentally acceptable.
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Thèses sur le sujet "Biologically potent molecules"

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Majumder, Sukdev. « Exploration of solvation consequences of some ionic liquids and biologically potent molecules prevailing in different liquid environments ». Thesis, University of North Bengal, 2022. http://ir.nbu.ac.in/handle/123456789/4758.

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Roy, Niloy. « Synthesis, characterization and innovative applications of inclusion complexes and nanocomposites of some biologically potent molecules ». Thesis, University of North Bengal, 2022. http://ir.nbu.ac.in/handle/123456789/4754.

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Yasmin, Ananya. « Investigation of Host Guest Inclusion Complexations and Diverse Interactions of Some Industrially and Biologically Potent Molecules in Assorted Phases by Physicochemical Methodologies ». Thesis, University of North Bengal, 2019. http://ir.nbu.ac.in/handle/123456789/2854.

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Biplab, Rajbanshi. « Investigation of host- guest inclusion complexation of some biologically potent molecules and solvent consequences of some food preservations with the manifestation of synthesis, characterization and innovative applications ». Thesis, University of North Bengal, 2020. http://ir.nbu.ac.in/handle/123456789/3963.

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Yasrebi, Kaveh [Verfasser], Andreas [Gutachter] Hilgeroth, Sibel Gutachter] Süzen et Michael [Gutachter] [Lalk. « Synthesis and biological evaluation of trisindolyl-cycloalkanes and bis-indolyl naphthalene small molecules as potent antibacterial and antifungal agents / Kaveh Yasrebi ; Gutachter : Andreas Hilgeroth, Sibel Süzen, Michael Lalk ». Halle (Saale) : Universitäts- und Landesbibliothek Sachsen-Anhalt, 2020. http://d-nb.info/1237685796/34.

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Chapitres de livres sur le sujet "Biologically potent molecules"

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Thakur, Shabnam. « RADIOPHARMACEUTICAL SCIENCES ». Dans Futuristic Trends in Pharmacy & ; Nursing Volume 2 Book 23, 342–47. Iterative International Publishers, Selfypage Developers Pvt Ltd, 2023. http://dx.doi.org/10.58532/v2bs23p1ch27.

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Nowadays all the fields of sciences such as chemistry, medicines, biology, and pharmacology exploiting the use of a radionuclide as medication or other biologically active molecule. These molecules are very potent and play a very big role in improving human life by treating many diseased conditions. The new techniques have been used in various nuclear drug procedures, the produced radiopharmaceuticals are used for both internal radiation (i.e., noninvasive scintigraphy imaging). This radioligand therapy (RLT), also known as noninvasive scintigraphy imaging. The design, synthesis, radiolabeling, biology, and preclinical assessment of the medicines, as well as their clinical use, are all taken into account during the creation of radiopharmaceuticals. Contributions could be made in the areas of targeted, pretargeted, and non-targeted radiopharmaceuticals, ranging from small molecules through peptides, peptidomimetics, antibodies, and their derivatives, to particles for use in gamma scintigraphy, such as single photon emission tomography (SPECT), positron emission tomography (PET), and endoradiotherapy. Strong interest exists in the fields of diagnostic imaging and (radio) pharmaceutical treatment that are supported by diagnostic imaging. It is also acceptable to take allied subjects including physics, dosimetry, radio pharmacy, and hybrid imaging
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Freedman, Robert. « Beyond the Dopamine Theory ». Dans The Madness Within Us, 141–50. Oxford University PressNew York, NY, 2009. http://dx.doi.org/10.1093/oso/9780195307474.003.0008.

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Abstract The dopamine theory of schizophrenia grew out of the profound effects of the neuroleptic drugs, and it has had the predictive value of guiding the design of ever more potent drugs. Chlorpromazine required a mean daily dose of 400 to 800 mg. Haloperidol, the most potent of the D2 dopamine receptor antagonists, was equally as effective in doses of 1 to 5 mg. There have been many attempts to find definitive biological evidence that there is increase in dopamine transmission by some mechanism in schizophrenia. Increased dopamine metabolism, altered dopamine receptors, and genetic deficits in any molecule related to dopamine have been difficult to substantiate by any technique of molecular biology or brain imaging. This lack of evidence fits with the clinical observation that schizophrenia is not cured by these drugs.
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Fields, Gregg B., et Janelle L. Lauer-Fields. « Principles and Practice of Solid-Phase Peptide Synthesis ». Dans Synthetic Peptides. Oxford University Press, 2002. http://dx.doi.org/10.1093/oso/9780195132618.003.0006.

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Peptides play key structural and functional roles in biochemistry, pharmacology, and neurobiology, and are important probes for research in enzymology, immunology, and molecular biology. The amino acid building blocks can be among the 20 genetically encoded L-residues, or else unusual ones, and the sequences can be linear, cyclic, or branched. It follows that rapid, efficient, and reliable methodology for the chemical synthesis of these molecules is of utmost interest. A number of synthetic peptides are significant commercial or pharmaceutical products, ranging from the sweet dipeptide L-Asp-L-Phe-OMe (aspartame) to clinically used hormones such as oxytocin, adrenocorticotropic hormone, calcitonin, and gonadotropin releasing hormone (GnRH) super-agonists. Synthesis can lead to potent and selective new drugs by judicious substitutions that change functional groups and/or conformations of the parent peptide. These include introduction of N- or C-alkyl substituents, unnatural or D-amino acids, side-chain modifications including sulfate or phosphate groups or carbohydrate moieties, and constraints such as disulfide bridges between half-cystines or side-chain lactams between Lys and Asp or Glu. Commercially important products that evolved from such studies include protease inhibitors, such as captopril and other angiotensin converting enzyme (ACE) inhibitors, peptidomimetic HIV protease inhibitors, and the somatostatin analog lanreotide. Most of the biologically or medicinally important peptides which are the targets for useful structure-function studies by chemical synthesis comprise under 50 amino acid residues, but occasionally a synthetic approach can lead to important conclusions about small proteins (full or domains) in the 100-200 residue size range. Methods for synthesizing peptides are divided conveniently into two categories: solution (classical) and solid-phase pep tide synthesis (SPPS). The classical methods have evolved since the beginning of the twentieth century, and they are described amply in several reviews and books (Wünsch, 1974; Finn and Hofmann, 1976; Bodanszky and Bodanszky, 1984; Goodman et al, 2001). The solid-phase alternative was conceived and elaborated by R. B. Merrifield beginning in 1959, and has also been covered comprehensively (Erickson and Merrifield, 1976; Birr, 1978; Barany and Merrifield, 1979; Stewart and Young, 1984; Merrifield, 1986; Barany et al., 1987, 1988; Kent, 1988; Atherton and Sheppard, 1989; Fields and Noble, 1990; Barany and Albericio, 1991; Fields et al., 1992; Gutte, 1995; Fields, 1997; Lloyd-Williams et al., 1997; Chan and White, 2000; Kates and Albericio, 2000).
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Rapley, Ralph. « Antibody Engineering and Immunotherapeutics ». Dans Molecular Biology and Biotechnology, 226–57. 7e éd. The Royal Society of Chemistry, 2021. http://dx.doi.org/10.1039/9781788017862-00226.

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Antibodies have been known for many years to be a powerful therapeutic molecule and have given rise to the ‘magic bullet’ approach to targeted therapy of disease. Significant advances in the discovery and development of monoclonal antibodies and hybridoma technology led to the first engineered antibody in 1984. Since then, hundreds of antibodies are now being used for treatment and many more are in clinical trials. This chapter focuses on the production of hybridomas, the development of antibody humanisation techniques, surface display strategies and transgenic techniques that all play a major role in monoclonal antibody production for use in immunotherapeutics. The ability to conjugate antibodies to toxins and drugs to allow the delivery of potent molecules to disease targets and the potential to produce antibody fragments such as scFvs and nanobodies is also introduced. Furthermore, advances in CDR (complementarity-determining region) analysis and the molecular techniques that allow the fine tuning of antibody specificity and affinity are also covered. There is no doubt that the new generation of biological therapeutics will continue to have a profound impact on the present and future treatment of disease and a number of examples are presented within the chapter.
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Gupta, Anushree. « An Overview of Gene Variants of Endothelin-1 : A Critical Regulator of Endothelial Dysfunction ». Dans Endothelial Dysfunction - A Novel Paradigm [Working Title]. IntechOpen, 2022. http://dx.doi.org/10.5772/intechopen.108108.

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Endothelial dysfunction (ED) is an early marker of development of cardiovascular diseases and is closely related to clinical events in patients with atherosclerosis and hypertension. Endothelin-1 (ET-1), a potent vasoconstrictor, and nitic oxide (NO), a potent vasodilator, produced in endothelial cells are leading molecules which regulate vascular function. Failure of the physiological balance between these two molecules, often aggravated by increased production and biological activity of ET-1, commonly reflects endothelial dysfunction. The role of endothelium-derived small molecules like ET-1 (among many) with diverse biological functions continues to fascinate researchers all over the world both for its evolutionary significance and its translational potential in disease biology. Studies on systems genetics in human endothelial cells have provided evidence supporting the possibility that predisposition to complex disease is manifested through noncoding common genetic variants that modify levels of target gene expression in endothelial cells. These studies highlight the importance genetic variants of regulatory molecules secreted by endothelial cells in health and disease. It is unlikely that a single-nucleotide polymorphism (SNP) would directly cause disease, but it would increase the genetic predisposition of individuals and can affect their responses to drugs and medications. The knowledge gained would help in the risk stratification and clinical management of patients with personalized medicine.
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Basu, Anamika, Piyali Basak et Anasua Sarkar. « Molecular-Docking-Based Anti-Allergic Drug Design ». Dans Pharmaceutical Sciences, 711–26. IGI Global, 2017. http://dx.doi.org/10.4018/978-1-5225-1762-7.ch027.

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Allergens are foreign proteins that when come in contact of part(s) of human body stimulate the production of immunoglobulin types of proteins (antibodies). These allergens react with antibodies (immunoglobulin type E or IgE) produces allergic reactions, also known as immediate-type hypersensitivity reactions. As much as 20% of the general population may be affected by grass pollen as a major cause of allergic disease. EXPB class of proteins are known in the immunological literature as group-1 grass pollen allergens Molecular docking method can be used to identify the predicated the interaction of pollen allergen EXPB1 (Zea m 1), a beta-expansin and group-1 pollen allergen from maize with IgE molecules of human. The World Health Organization recognised allergen immunotherapy, as therapeutics for allergic diseases. RNA Interference (RNAi) is a biological process in which RNA molecules e.g. Small Interfering RNAs (siRNAs) inhibit gene expression, by cleavage and destruction of specific mRNA molecules. Use of Small Interfering RNA (siRNA) is a novel method in the induction of RNA Interference (RNAi), which is a potent method for therapeutics of allergic reactions. Due to various effects of STAT 6 proteins during hypersensitivity reactions caused by pollen allergens, mRNA of STAT6 gene is selected as target gene for allergy therapeutics via Post-Transcriptional Gene Silencing (PTGS). Using molecular docking study a specific sense siRNA is identified as anti allergic drug to treat allergic asthma during immediate type of hypersensitivity reaction, caused by Zea m 1 pollen allergen.
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Basu, Anamika, Piyali Basak et Anasua Sarkar. « Molecular-Docking-Based Anti-Allergic Drug Design ». Dans Advances in Medical Technologies and Clinical Practice, 232–48. IGI Global, 2016. http://dx.doi.org/10.4018/978-1-5225-0362-0.ch009.

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Allergens are foreign proteins that when come in contact of part(s) of human body stimulate the production of immunoglobulin types of proteins (antibodies). These allergens react with antibodies (immunoglobulin type E or IgE) produces allergic reactions, also known as immediate-type hypersensitivity reactions. As much as 20% of the general population may be affected by grass pollen as a major cause of allergic disease. EXPB class of proteins are known in the immunological literature as group-1 grass pollen allergens Molecular docking method can be used to identify the predicated the interaction of pollen allergen EXPB1 (Zea m 1), a beta-expansin and group-1 pollen allergen from maize with IgE molecules of human. The World Health Organization recognised allergen immunotherapy, as therapeutics for allergic diseases. RNA Interference (RNAi) is a biological process in which RNA molecules e.g. Small Interfering RNAs (siRNAs) inhibit gene expression, by cleavage and destruction of specific mRNA molecules. Use of Small Interfering RNA (siRNA) is a novel method in the induction of RNA Interference (RNAi), which is a potent method for therapeutics of allergic reactions. Due to various effects of STAT 6 proteins during hypersensitivity reactions caused by pollen allergens, mRNA of STAT6 gene is selected as target gene for allergy therapeutics via Post-Transcriptional Gene Silencing (PTGS). Using molecular docking study a specific sense siRNA is identified as anti allergic drug to treat allergic asthma during immediate type of hypersensitivity reaction, caused by Zea m 1 pollen allergen.
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Martin, Y. C., M. G. Bures, E. A. Danaher, J. DeLazzer, K. H. Kim, I. Lico et P. A. Pavlik. « 3D DESIGN AND POTENCY FORECAST OF BIOLOGICALLY ACTIVE MOLECULES ». Dans Computer Aided Innovation of New Materials II, 1117–20. Elsevier, 1993. http://dx.doi.org/10.1016/b978-0-444-89778-7.50057-8.

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Saltzman, W. Mark. « Drug Modification ». Dans Drug Delivery. Oxford University Press, 2001. http://dx.doi.org/10.1093/oso/9780195085891.003.0014.

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Previous chapters present the characteristics of drug movement through the body. Diffusion is an essential mode of transport at the microscopic scale; concentration gradients drive a substantial fraction of the molecular movements within cells and the extracellular space. The confinement and regulated passage of molecules within compartments of a tissue or cell is also essential for function; membranes confine molecules to spatial locations and regulate transport between these isolated spaces (Chapter 5). Membranes frequently are the major obstacles to the entry or distribution of therapeutic compounds (Chapter 7). Therefore, much of the effort in drug design and drug delivery is devoted to overcoming these diffusional or membrane barriers. This chapter describes strategies for manipulating agents in order to increase their biological activity. The sections orbit a central assumption: i.e., agents can be modified to make analogous agents (analogs), which are chemically distinct from the original compound, but produce a similar biological effect. Nature uses a similar strategy, called “biotransformation” to assure elimination of many toxic compounds and drugs. Substantial chemical modification is often needed in order to impact physical properties that influence drug distribution such as stability or solubility; the challenge of drug modification is to identify chemical features that can be changed without sacrificing biological activity. Often, our understanding of the relationship between chemical structure and biological function for an agent is incomplete, making the rational production of analogs difficult. Drug modifications are frequently directed at altering properties that influence the concentration of the compound (i.e., its solubility), the duration of action (which is usually related to its stability in tissue), or the ability of drug molecules to move between compartments in tissues (which is often related to its permeability in membranes). A chemical modification can effect multiple properties, so these divisions are frequently not as distinct as the section headings suggest. Many agents are protected from degradation within tissues by binding. Binding provides a mechanism for sequestering an unstable or potent compound within a region of a tissue. Protective binding occurs frequently within the plasma and extracellular matrix (ECM); the complex molecular composition of these tissues provides many potential binding sites.
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Kumari, Archana, et Rajesh K. Singh. « Morpholine : Pharmacophore Modulating Pharmacokinetic Properties of Anticancer Leads ». Dans Key Heterocyclic Cores for Smart Anticancer Drug–Design Part II, 137–73. BENTHAM SCIENCE PUBLISHERS, 2022. http://dx.doi.org/10.2174/9789815040043122020008.

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The morpholine ring is considered the most preferred and versatile heterocylic ring in medicinal chemistry due to its distinctive mechanistic activities that give it various biological activities. The eminence of the morpholine ring to modulate the pharmacokinetic properties of the compound, further makes it a fundamental pharmacophore in developing lead molecules. Multi-drug resistance in cancer leads to discovering selective and potent chemotherapeutic agents. Researchers are designing and synthesizing morpholine derivatives as potential anticancer drugs those act by targeting various signaling pathways driven by various protein kinases in the cell, i.e. Ras-Raf-MEK-ERK (ERK) and PI3K/Akt/mTOR, thereby inhibiting cell proliferation and growth. The potency of natural and synthetic derivatives of morpholine makes it a drug of choice for cancer treatment. Many of the morpholine containing anticancer drugs are under clinical trials. Hence, morpholine ring synthesis also becomes a central target for various scientists using green synthesis by straightforward one-step methods. A substantial literature is available on synthetic techniques of morpholine and substituted morpholine. The present chapter updates diverse new synthetic strategies of the morpholine ring and morpholine derivatives with potent anticancer activity. The chapter will also highlight the clinical data of morpholine derivatives with anticancer activity and mechanism of action. The latest information on novel anticancer morpholine derivatives with structural activity relationship (SAR) is also included. This chapter provides information about the necessary structural modifications required in drugs' chemical structure and contribute to the anticancer drug discovery program.
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Actes de conférences sur le sujet "Biologically potent molecules"

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Ragno, Rino, et Alessio Ragno. « db.3d-qsar.com. The first 3D QSAR models database ». Dans 2nd International Conference on Chemo and Bioinformatics. Institute for Information Technologies, University of Kragujevac, 2023. http://dx.doi.org/10.46793/iccbi23.051r.

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Field-Based Three-Dimensiona Quantitative Strucutere-Activity Relationships (FB 3D QSAR) comprise computational approaches used in drug design and molecular modeling to analyze the relationship between the three-dimensional structure of a list of molecules (described by molecular interaction fields) and their associated biological activities (BAs). It aims to understand how different structural features of the molecules contribute to enhancing or lowering the biological potency. The process of FB 3D QSAR involves several steps. First, a dataset of structurally diverse molecules with known BAs is selected. Then, their three-dimensional structures are generated using computational methods. Next, in the classical form of Cramer [1], sterical and electrostatic molecular interaction fields (MIFs) are calculated and as a final step a mathematical model is built through the correlation of BAs with MIFs by means of projection of latent structures (PLS) algorithm. With our interest in making 3D QSAR accessible to all as done with the www.3d-qsar.com [2] db.3d-qsar.com, the first publicly available database of 3D QSAR models, is presented in which the user can insert or draw a molecule and predict its potency against an available target. All the models available on db.3d-qsar.com have been heavily optimized in prediction power through a semi-systematic pretreatment and parameter selection procedure by initially dividing the datasets into training (80%) and prediction (20%) sets. Each published model was and will be prepared by a selection among thousands of alignment trials. The selected models were finally characterized using a validation set compiled with molecules taken from the ChEMBL database. At the time of writing more than 40 models associated to more than 30 different pharmacological targets have been prepared and are ready to be used. At the time of the presentation db.3d-qsar.com will be accessible to the public and during the presentation its features will be shown.
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Hussein, Ola, Feras Alali, Ala‐Eddin Al Mustafa et Ashraf Khalil. « Development of Novel Chalcone Analogs as Potential Multi-Targeted Therapies for Castration-Resistant Prostate Cancer ». Dans Qatar University Annual Research Forum & Exhibition. Qatar University Press, 2021. http://dx.doi.org/10.29117/quarfe.2021.0114.

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Prostate cancer (PCa) is the second most frequently diagnosed malignancy, as well as a leading cause of cancer-related mortality in men globally. Despite the initial response to hormonal targeted therapy, the majority of patients ultimately progress to a lethal form of the disease, castration-resistant prostate cancer (CRPC). Therefore, the objective of this study was to discover and develop novel treatment modalities for CRPC. Chalcones are among the highly attractive scaffolds being investigated for their antitumor activities. A library of 26 chalcone analogs were designed, synthesized and evaluated as potential therapies for CRPC. The design was guided by in-silico ADMET prediction in which analogs with favorable drug-likeness properties were prioritized. The new compounds were synthesized, purified and characterized by extensive structural elucidation studies. The compounds in vitro cytotoxicity was evaluated against two androgen receptor (AR)-negative prostate cancer cell lines (PC3 and DU145). Among the tested compounds, pyridine containing analogs (13, 15 and 16) showed potent antiproliferative activities with IC50 values ranging between 4.32-6.47 µM against PC3 and DU145 cell lines. Detailed biological studies of the lead molecule 16 revealed that it can significantly induce apoptosis through upregulation of Bax and downregulation of Bcl-2. In addition, compound 16 potently inhibited colony formation and reduced cell migration of AR-negative PCa cell lines (PC3 and DU145). The molecular pathway analysis showed that the anticancer activity of compound 16 is associated with blocking of ERK1/2 and Akt activities. Furthermore, compound 16 inhibited angiogenesis in the chick chorioallantoic membrane (CAM) model as compared to control. Structure-activity relationship study revealed that the cytotoxicity could dramatically improve via changing the methoxylation pattern by more than 2-folds (IC50 << 2.5 μM). These results indicate that pyridine-based chalcones could serve as promising lead molecules for the treatment of CRPC; thus, further in vitro and in vivo studies are warranted.
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Hussein, Ola, Feras Alali, Ala-Eddin Al Moustafa et Ashraf Khalil. « Design, Synthesis and Biological Evaluation of Novel Chalcone Analogs as Potential Therapeutic Agents for Castration-Resistant Prostate Cancer ». Dans Qatar University Annual Research Forum & Exhibition. Qatar University Press, 2020. http://dx.doi.org/10.29117/quarfe.2020.0179.

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Prostate cancer (PCa) is the second most frequently diagnosed malignancy, as well as a leading cause of cancer-related mortality in men globally. Despite the initial response to hormonal targeted therapy, the majority of patients ultimately progress to a lethal form of the disease, termed as castration-resistant prostate cancer (CRPC), which currently lacks curative therapeutic options and is associated with poor prognosis. Therefore, the development of novel treatment modalities for PCa is urgently needed. Chalcones, also known as 1,3-diphenyl-2-propen-1-ones, are among the highly attractive scaffolds being investigated for their antitumor activities. Three series of 18 cyclic (tetralone-based) and two acyclic chalcone analogs, in which ring B was either substituted with nitrogen mustard or replaced by pyrrole or pyridine heterocyclic rings, were designed, synthesized and evaluated as potential therapies for CRPC. Compounds were synthesized by Claisen-Schmidt condensation reaction, purified using columnchromatography or recrystallization and characterized by 1H-NMR, 13C-NMR and LC-MS. The compounds' in-vitro cytotoxicity was evaluated against three prostate cancer cell lines (PC3, DU145, and LNCaP). Among the tested compounds, OH14, OH19 and OH22 showed potent antiproliferative activities at low micromolar levels with IC50 values ranging between 4.4 and 10 µM against PC3 and DU145 cell lines. Detailed biological studies of the lead molecule OH19 revealed that it significantly induces apoptosis through upregulation of Bax and downregulation of BCL-2. In addition, OH19 potently inhibits colony formation and reduces cell migration of androgen-independent PCa cell lines (PC3 and DU145). The molecular pathway analysis show that the anticancer activity of OH19 is associated with attenuation in the phosphorylation of Akt and ERK. Furthermore, OH19 inhibits blood vessel formation in the chick chorioallantoic membrane (CAM) model as compared to control. These results indicate that OH19 could serve as a potential promising lead molecule for the treatment of CRPC and thus, further in-vitro and invivo studies are warranted.
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Grajdieru, Cristina. « Molecular identification of Aflatoxin-producing aspergillus strains in maize seed-material ». Dans International Scientific Symposium "Plant Protection – Achievements and Prospects". Institute of Genetics, Physiology and Plant Protection, Republic of Moldova, 2020. http://dx.doi.org/10.53040/9789975347204.66.

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Toxigenic fungi are part of soil microbiota and natural inhabitants of agrocenosises and crops. Aflatoxins produced by several Aspergillus species are hazardous biological compounds known as potent carcinogens. Using PCR-based assays, a successful identification of toxigenic A. flavus and A. parasiticus strain was performed. Fungal genome sequences associated with aflatoxin production as target sequences were proved to be effective for identification of toxigenic Aspergillus species.
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Frame, Sheelagh, Claire Aspinall, Robert O'Neil, Jonathan Hollick, Stephen Taylor, Ted Hupp, David Blake et Daniella I. Zheleva. « Abstract 2814 : Potent and selective small molecule inhibitors of polo-like kinase 1 : Biological characterization ». Dans Proceedings : AACR 103rd Annual Meeting 2012‐‐ Mar 31‐Apr 4, 2012 ; Chicago, IL. American Association for Cancer Research, 2012. http://dx.doi.org/10.1158/1538-7445.am2012-2814.

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Libby, Peter, Stephen J. C. Warner et Louis K. Birinyi. « THE VESSEL WALL AS A SOURCE OF VASORHGOLATORY AND IMMDNOSTIMOLATORY CYTOKINES ». Dans XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1643982.

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The cytokines Interleukin-1 (IL-1) and Tumor Necrosis Factor (TNF, also known as cachectin) exhibit multiple effects on circulating blood cells and cells of the blood vessel wall. For example, these mediators elicit a coordinated Drogram of functions of endothelial cells (EC) that promotes blood coagulation and thrombosis, and lead to clot stabilization. Furthermore, IL-1 and TNF promote adherence to vascular endothelium of leukocytes of many classes.Thus, these cytokines are likely to be involved in signaling the pathologic changes in blood vessels that characterize a number of inflammatory or infectious processes. These two cytokines were originally isolated frcm activated human mononuclear phagocytes, hence their comnon designation as monokines and the terminology "interleukin". However, recent findings have broadened this concept considerably. It is now clear that many cell types can produce IL-1-1ike activity.Several groups showed that human vascular EC can secrete material that stimulates proliferation of thymocytes incubated with suboptima1 doses of the mitogenic lectin phytohemagglutinin, a typical acitivty of IL-1 (thymocyte costimulation).Two related but distinct genes cloned frcm human peripheral blood monocytes encode IL-1 molecules. In human blood monocytes stimulated with bacterial lioopolysaccharide (LPS) IL-1 beta (pi ∼ 7) is the major form expressed while IL-1 alpha (pi ∼ 5) is the less abundant species secreted by human monocytes under these conditions. We found that EC and smooth muscle cells (SMC) isolated from adult human vessels can express these same IL-1 genes. LPS, a standard stimulus to IL-1 secretion in the monocyte, caused accumulation of IL-1 beta mRNA in both vascular cell types. Endothelial cells frcm adult human vessels also contained IL-1 alpha mRNA when treated with LPS in the presence of cycloheximide and LPS-stimulated smooth muscle cells contained RNA that hybridized with an IL-1 alpha cDNA probe as well. Although both vascular cell types can transcribe these IL-1 genes, the time course of this response differs. LPS induced IL-1 beta mRNA production by SMC maximally at 4-6 hr., whereas maximal IL-1 induction by LPS in EC occured 1 day after initiation of the exposure. Actinanycin D (1 ug/ml) blocked 3H-uridine incorporation into macromolecules by > 95% in both EC & SMC, and prevented the LPS-induced increases in IL-1 mRNA levels in these cells. This result suggests that this potentially injurious stimulus causes IL-1 mRNA accumulation by an increase in rates of transcription. These LPS-induced increases in IL-1 mRNA levels corresponded to production of biologically active IL-1 determined as thymocyte costimulation activity. Interestingly, gel filtration experiments revealed a molecular weight of around 22kD for both SMC and EC-derived IL-1 secreted into culture medium in response to LPS. This molecular weight contrasts with the 17 kD species which is the fully processed product secreted frcm activated human monocytes. A possible explanation for this disparity is that the vascular cells secrete a partially processed intermediate form of mature IL-1. Other stimuli for IL-1 mRNA accumulation and secretion of biological activity include TNF and IL-1 itself. Recombinant human INF (≥ 10 ng/ml) increased IL-1 beta mRNA levels in EC & SMC, and caused the EC & SMC to release IL-1-1 ike thymocyte costimulation activity. Of interest is the recent observation that IL-1 itself can stimulate expression of IL-rl genes in vascular wall cells. Both IL-1 aloha and beta can increase IL-1 beta mRNA content in EC & SMC. Hris observation was confirmed with homogenous IL-1 prepared by recombinant DNA technologies (rIL-1). These findings raise the possibility of a novel positive feedback loop in vascular pathophysiology. We also found that rIL-1 alpha or beta also induced the production of prostaglandin E2 (PGE2) by both vascular SMC & EC. This prostanoid, induced by IL-1, inhibits thymocyte _ proliferation. Thus, IL-1 not only induced its own expression but increased production of this immunosuppressive prostanoid. This mechanism provides a potential negative control loop in regulation of the local immune response in blood vessels. Vie conclude that these cells of the blood vessel wall are a source of the potent vasoregulatory and immune mediators IL-1 alpha and beta. Since IL-1 influences the thrombotic, hemostatic, and fibrinolytic functions of endothelium, as well as other responses to acute injury, our findings suggest novel local control mechanisms that may be important in a variety of pathologic states.
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Haigwood, N., E.-P. Pâques, G. Mullenbach, G. Moore, L. DesJardin et A. Tabrizi. « IMPROVEMENT OF T-PA PROPERTIES BY MEANS OF SITE DIRECTED MUTAGENESIS ». Dans XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1643841.

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The clinical relevance of tissue-plasminogen-activator (t-PA) as a potent thrombolytic agent has recently been established. It has however been recognized that t-PA does not fulfill all conditions required for an ideal thrombolytic pharmaceutical agent; for example, its physiological stability and its short half life in vivo necessitate the use of very large clinical doses. We have therefore attempted to develop novel mutant t-PA proteins with improved properties by creating mutants by site-directed mutagenesis in M13 bacteriophage. Seventeen mutants were designed, cloned, and expressed in CHO cells. Modifications were of three types: alterations to glycosylation sites, truncations of the N- or C-termini, and amino acids changes at the cleavage site utilized to generate the two chain form of t-PA. The mutant proteins were analyzed in vitro for specific activity, fibrin dependence of the plasminogen activation, fibrin affinity, and susceptibility to inhibition by PAI.In brief, the results are: 1) some unglycosylated and partially glycosylated molecules obtained by mutagenesis are characterized by several-fold higher specific activity than wild type t-PA; 2) truncation at the C-terminus by three amino acids yields a molecule with increased fibrin specificity; 3) mutations at the cleavage site lead zo a decreased inhibition by PAI; and 4) recombinants of these genes have been constructed and the proteins were shown to possess multiple improved properties. The use of site directed mutagenesis has proved to be a powerful instrument to modulate the biological properties of t-PA.
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Dumas, Sabrina, Lei Du-Cuny, Sylvestor Moses, Zuohe Song, Shuxing Zhang et Emmanuelle J. Meuillet. « Abstract 2166 : In silico identification and biological evaluation of potent small molecule inhibitors targeting GAB1 pleckstrin homology domain ». Dans Proceedings : AACR 103rd Annual Meeting 2012‐‐ Mar 31‐Apr 4, 2012 ; Chicago, IL. American Association for Cancer Research, 2012. http://dx.doi.org/10.1158/1538-7445.am2012-2166.

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Hardwicke, Mary Ann, Hong Lu, Lusong Luo, Melody Diamond, Chiu‐Mei Sung, Jeffrey D. Carson, Ramona Plant et al. « Abstract C63 : Biological characterization of GSK2126458, a novel and potent inhibitor of phosphoinositide 3‐kinase and the mammalian target of rapamycin (mTOR) ». Dans Abstracts : AACR-NCI-EORTC International Conference : Molecular Targets and Cancer Therapeutics--Nov 15-19, 2009 ; Boston, MA. American Association for Cancer Research, 2009. http://dx.doi.org/10.1158/1535-7163.targ-09-c63.

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Tek, Erhan, et Nizami Duran. « Efficacy of Capsaicin on Cell Adhesion and Invasion of Oral Pathogens ». Dans The 9th International Conference on Advanced Materials and Systems. INCDTP - Leather and Footwear Research Institute (ICPI), Bucharest, Romania, 2022. http://dx.doi.org/10.24264/icams-2022.iii.19.

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Streptococcus pyogenes, Streptococcus mutans, and Candida albicans are important human pathogens and their infections in the mouth, mouth, and throat are important. Prophylaxis against oral and respiratory tract infections is of great importance in terms of both reducing the use of antibiotics and lowering the infection frequency. This study investigated the antimicrobial activity of Capsaicin against S. mutans, C. albicans, and S. pyogenes. Non-cytotoxic concentration of Capsaicin was determined in the Vero cell line by the MTT method. Efficacy studies were performed within these determined non-cytotoxic concentrations. The efficacy of single and different combinations of these three biological components on cell adhesion and invasion. The non-toxic concentration of capsaicin on Vero cells was <1.35 µg/ml. Capsaicin exhibited significant antimicrobial activity against S. pyogenes, S. mutans, and C. albicans. Moreover, capsaicin was statistically significantly effective against host cell adhesion and invasion against S. mutans, S. pyogenes and C. albicans compared to the control group. The results showed that capsaicin is a highly potent antibacterial agent against S. pyogenes, and S. mutans, as well as an important prophylactic agent for fungal infections. As a result, we think that capsaicin is a useful molecule for the provision and maintenance of both respiratory diseases and oral health.
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