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Artykuły w czasopismach na temat "Pyrazolopyrimidines"
George, CFP. "Pyrazolopyrimidines". Lancet 358, nr 9293 (listopad 2001): 1623–26. http://dx.doi.org/10.1016/s0140-6736(01)06656-9.
Pełny tekst źródłaWald, Jiri, Marion Pasin, Martina Richter, Christin Walther, Neann Mathai, Johannes Kirchmair, Vadim A. Makarov i in. "Cryo-EM structure of pleconaril-resistant rhinovirus-B5 complexed to the antiviral OBR-5-340 reveals unexpected binding site". Proceedings of the National Academy of Sciences 116, nr 38 (28.08.2019): 19109–15. http://dx.doi.org/10.1073/pnas.1904732116.
Pełny tekst źródłaLu, Shi-Han, Po-Lin Liu i Fung Fuh Wong. "Vilsmeier reagent-mediated synthesis of 6-[(formyloxy)methyl]-pyrazolopyrimidines via a one-pot multiple tandem reaction". RSC Advances 5, nr 58 (2015): 47098–107. http://dx.doi.org/10.1039/c5ra07707a.
Pełny tekst źródłaAgrebi, Asma, Fatma Allouche, Hamadi Fetoui i Fakher Chabchoub. "Synthesis and biological evaluation of new pyrazolo[3,4-d]pyrimidine derivatives". Mediterranean Journal of Chemistry 3, nr 2 (13.05.2014): 864. http://dx.doi.org/10.13171/mjc.3.2.2014.13.05.23agrebi.
Pełny tekst źródłaElnagdi, Mohamed Hilmy, Ahmed Hafiz Husein Elghandour, Mohamed Kamal Ahmed Ibrahim i Ibrahim Saad Abdel Hafiz. "Studies with Polyfunctionally Substituted Heterocycles: Synthesis of New Pyridines, Naphtho[1,2-b]pyrans, Pyrazolo[3,4-b]pyridines and Pyrazolo[l,5-a]pyrimidines". Zeitschrift für Naturforschung B 47, nr 4 (1.04.1992): 572–78. http://dx.doi.org/10.1515/znb-1992-0419.
Pełny tekst źródłaKolosov, Maksim A., Dmitriy A. Beloborodov, Valeriy D. Orlov i Victor V. Dotsenko. "Catalyst-free Biginelli-type synthesis of new functionalized 4,7-dihydropyrazolo[1,5-a]pyrimidines". New Journal of Chemistry 40, nr 9 (2016): 7573–79. http://dx.doi.org/10.1039/c6nj00336b.
Pełny tekst źródłaEl-Dean, Adel M. Kamal, i Maisa E. Abdel-Moneam. "Synthesis of Pyrimidines, Thienopyrimidines, and Pyrazolopyrimidines". Phosphorus, Sulfur, and Silicon and the Related Elements 177, nr 12 (1.12.2002): 2745–51. http://dx.doi.org/10.1080/10426500214894.
Pełny tekst źródłaWeitensteiner, Sabine B., Johanna Liebl, Vladimir Krystof, Libor Havlíček, Tomáš Gucký, Miroslav Strnad, Robert Fürst, Angelika M. Vollmar i Stefan Zahler. "Trisubstituted Pyrazolopyrimidines as Novel Angiogenesis Inhibitors". PLoS ONE 8, nr 1 (15.01.2013): e54607. http://dx.doi.org/10.1371/journal.pone.0054607.
Pełny tekst źródłaRice, Kenneth D., Moon H. Kim, Joerg Bussenius, Neel K. Anand, Charles M. Blazey, Owen J. Bowles, Lynne Canne-Bannen i in. "Pyrazolopyrimidines as dual Akt/p70S6K inhibitors". Bioorganic & Medicinal Chemistry Letters 22, nr 8 (kwiecień 2012): 2693–97. http://dx.doi.org/10.1016/j.bmcl.2012.03.011.
Pełny tekst źródłaAhmed, Sayed A., Ahmed M. Hussein, Walaa G. M. Hozayen, Ahmed H. H. El-Ghandour i Abdou O. Abdelhamid. "Synthesis of some pyrazolopyrimidines as purine analogues". Journal of Heterocyclic Chemistry 44, nr 4 (lipiec 2007): 803–10. http://dx.doi.org/10.1002/jhet.5570440408.
Pełny tekst źródłaRozprawy doktorskie na temat "Pyrazolopyrimidines"
Scammells, Peter J., i n/a. "Pyrazolo(3,4-d)Pyrimidines and adenosine receptors: a structure/activity study". Griffith University. Division of Science and Technology, 1990. http://www4.gu.edu.au:8080/adt-root/public/adt-QGU20050826.141630.
Pełny tekst źródłaScammells, Peter. "Pyrazolo(3,4-d)Pyrimidines and adenosine receptors: a structure/activity study". Thesis, Griffith University, 1990. http://hdl.handle.net/10072/365214.
Pełny tekst źródłaThesis (PhD Doctorate)
Doctor of Philosophy (PhD)
Division of Science and Technology
Full Text
Le, Corre Laurent. "Synthèse et évaluation biologique d’inhibiteurs de FGFR3 de structure pyrazolooxadiazole, pyrido- et pyrazolopyrimidine". Thesis, Paris 5, 2012. http://www.theses.fr/2012PA05P636.
Pełny tekst źródłaFGFR3 is a cellular receptor involved in many human biological processes. Deregulated tyrosine kinase activity of the FGFR3 is at the origin of abnormal bone growth and some cancers (multiple myeloma, bladder). Blocking this receptor by ATP competitive inhibitors may constitute an interestingtherapeutic approach. The first part of this thesis concerned the preparation of analogues of PD173074, a nanomolar inhibitor of FGFR3, stemming from the industry. Based on pyrido [2,3-d] pyrimidine skeleton, a library of triazoles was obtained via copper (I)-catalyzed 1,3-dipolar cycloaddition. Among the 27 analogues synthesized, the best inhibitor restores bone growth of dwarf mice femurs ex vivo. In a second part, we have developed two new series of inhibitors based on pyrazolooxadiazole and pyrazolo [4,3-d] pyrimidine skeletons, derived from a common pyrazole precursor. Rapid and efficient microwave procedures were used to yield the target compounds. The study of structure-activity relationships, performed on sixty compounds, was confirmed by molecular modeling. The most active compound has a submicromolar IC50 value
Cardoso, Inês Sofia Soares Gomes Lains. "Design and synthesis of a novel pyrazolopyrimidine compound as a potential kinase inhibitor". Master's thesis, 2016. http://hdl.handle.net/10451/34606.
Pełny tekst źródłaCancer is a generic term for a group of diseases in which abnormal cells have a fast and uncontrolled growth and proliferation, invading neighbouring tissues and spreading to parts of the body different from where it started. Cancer is placed second at the most important causes of death and morbidity in Europe and accounts for 1 in every 7 deaths worldwide, which is more than HIV, tuberculosis and malaria combined. Furthermore, the number of new cases worldwide is expected to rise by about 70% over the next 20 years due to the growth and aging of the population. Nowadays, there are several options of treatment available for different types of cancer. However, current treatment modalities remain inadequate and in need of improvement regarding selectivity, potency and toxicity. For this reason, both academia and pharmaceutical industry have shown interest in deeply investigating carcinogenesis at a molecular level, improving existing drugs and discovering new compounds for cancer treatment. Given the role of proteins kinases and phosphorylation processes in carcinogenesis by driving many of the hallmark phenotypes of cancer biology, kinases are privileged targets of new antineoplasic therapies and pharmacological tools have been developed to inhibit protein phosphorylation. Recently, several kinase inhibitors have been studied and approved for the treatment of some types of cancer, such as Imatinib, Sorafenib, among others. Among kinases inhibitors, pyrazolopyrimidines-derived compounds have been investigated and are used as treatment for several diseases, acting like antineoplasic, antivirals, and tuberculostatic agents, among others. Different kinase inhibitors with pyrazolopyrimidines as central core structure were studied and produced. The aim of this thesis was to synthesize a pyrazolo[3,4-d]pyrimidine derivative chemically designed as a hybrid of two previously synthesized compounds containing the mentioned central core structure and which had good and complementary results on the IC50 test against subfamilies of kinases, suggesting an improvement in selectivity and efficacy. One part of each of the previously studied molecules were synthesized separately and attached to each other through a Suzuki-Miyaura cross-coupling reaction.
Cancro é um termo genérico que engloba um grupo de doenças nas quais células anormais crescem e proliferam rápida e descontroladamente, invadindo tecidos circundandes e outras partes do corpo distantes do local de origem. O cancro é a segunda causa de morte e morbilidade na Europa e é responsável por 1 em cada 7 mortes a nível mundial, representando mais do que HIV, tuberculose e malária no seu conjunto. Além disso, o número de novos casos, numa perspectiva mundial, é esperado que cresça em, aproximadamente, 70% nos próximos 20 anos, devido ao crescimento e envelhecimento da população. Actualmente, estão disponíveis várias opções de tratamento para diferentes tipos de cancro. No entanto, as modalidades actuais de tratamento permancem inadequadas e por melhorar, em relação à selectividade, potência e toxicidade. Por esta razão, a academia e a indústria farmacêutica têm demonstrado interesse em investigar a carcinogénese a um nível molecular, de forma a aperfeiçoar fármacos já existentes e a descobrir novos compostos para o tratamento do cancro. Considerando o papel das proteínas cinases e dos processos de fosforilação na carcinogénese, por conduzir muitos dos fenótipos característicos da biologia do cancro, as cinases representam um alvo priveligiado de novas terapias antineoplásicas e têm sido desenvolvidas ferramentais farmacológicas para inibir a fosforilação proteica. Recentemente, vários inibidores de cinases têm sido estudados e aprovados para o tratamento de alguns tipos de cancro, como por exemplo Imatinib, Sorafenib, entre outros. De entre os inibidores de cinases, os compostos derivados de pirazolo-pirimidinas têm sido investigados e são utilizados como tratamento para diversas doenças, actuando como antineoplásicos, antivirais e agentes tuberculoestáticos, entre outros. Foram estudados diferentes inibidores de cinases com o núcleo estrutural constituído por pirazolo-pirimidinas. O objectivo da presente tese consistiu na síntese de um derivado de pirazolo[3,4-d]pirimidina, quimicamente desenhado como um híbrido de dois compostos previamente sintetizados que contêm o mencionado núcleo estrutural e que apresentaram bons resultados, porém complementares, no teste de IC50 contra subfamílias de cinases, sugerindo a necessidade de melhoria quanto à selectividade e eficácia. Uma parte de cada uma das moléculas previamente estudadas foram sintetizadas separadamente e ligadas através de uma reacção de acoplamento de Suzuki-Miyaura.
Chang, Hsin-Wen, i 張馨文. "A 3D-QSAR Study and Spatial Relation of Pyrazolopyrimidine Analogs and Their Target Protein mTOR". Thesis, 2011. http://ndltd.ncl.edu.tw/handle/22976125865108904445.
Pełny tekst źródła國立高雄大學
生物科技研究所
99
mTOR (mammalian target of rapamycin), a key regulator of growth, metabolism, and proliferation, exists as two forms of protein complexes, mTORC1 (mammalian target of rapamycin complex 1) and mTORC2 (mammalian target of rapamycin complex 2). Since mTORC1 and mTORC2 are highly involved in mediation of PI3K (phosphoinositol 3-kinase) signaling pathways that are deregulated in human tumors, they have been recognized as cancer treatment targets. According to the inhibition domains, mTOR inhibitors are categorized into rapamycin-binding domain inhibitors and of kinase domain (ATP-binding domain) inhibitors. The former targets at mTORC1, whereas the latter, which has been more widely studied in recent years, targets at both mTORC1 and mTORC2. Because of close similarity between kinase domains of mTOR and PI3K, inhibitors toward mTOR inevitably show certain degree of inhibition on PI3K. Delicate design of mTOR inhibitors is expected to achieve a higher therapeutic index for enhanced clinical efficacy. Herein 3D-QSAR (three-dimensional quantitative structure-activity relationship) modeling is applied to investigate 83 pyrazolopyrimidine derivatives, which were published in 2009 and expected to serve as selective mTOR kinase domain inhibitors by Wyeth Research. Due to the lack of known mTOR structure, homology method is adopted to build mTOR in complex with one studied compound to provide details of possible binding mode and further to be correlated with the 3D-QSAR models. The constructed models suggest that R1 with a urea-modified benzene moiety enhances the hydrogen bonding interaction with mTOR Asp2195, whereas R2 carrying a piperidine in connection with a pyridine boosts the electrostatic interaction with mTOR His2247. On the other hand, the size of substituent on R1 and the connector between piperidine and pyridine on R2 play essential roles in PI3K/mTOR selectivity.
Części książek na temat "Pyrazolopyrimidines"
Patrick, Graham. "Pyrazolopyrimidines". W Medicinal Chemistry, 241–44. Taylor & Francis, 2019. http://dx.doi.org/10.1201/9780429188572-54.
Pełny tekst źródłaElnagdi, Mohamed Hilmy, Mohamed Rifaat Hamza Elmoghayar i Galal Eldln Hamza Elgemeie. "Chemistry of Pyrazolopyrimidines". W Advances in Heterocyclic Chemistry Volume 41, 319–76. Elsevier, 1987. http://dx.doi.org/10.1016/s0065-2725(08)60164-6.
Pełny tekst źródłaStreszczenia konferencji na temat "Pyrazolopyrimidines"
Weiss, Andreas, Thomas Radimerski, Daniel Wyss, Rita Andraos, Alexandra Buhles, Dario Sterker, Jean Quancard i in. "Abstract 1879: Pyrazolopyrimidines as novel selective allosteric MALT1 inhibitors with in vivo activity in ABC-DLBCL". W Proceedings: AACR Annual Meeting 2018; April 14-18, 2018; Chicago, IL. American Association for Cancer Research, 2018. http://dx.doi.org/10.1158/1538-7445.am2018-1879.
Pełny tekst źródłaZask, Arie, Joshua Kaplan, Kevin Curran, Jeroen C. Verheijen, David J. Richard, Natasja Brooijmans, Eric Bennett i in. "Abstract B145: Highly selective pyrazolopyrimidine mTOR inhibitors with profoundin vivoantitumor activity". W 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-b145.
Pełny tekst źródłaNegmeldin, Ahmed T., Mohammed K. AbdElhameid, Dalia Y. Alsaeedy, Fatiha Hammed, Rasha M. Allam, Walid El-Sayed i Ahmed M. Al-Abd. "Abstract LB-236: Design, synthesis, and assessment of anticancer properties of pyrazolopyrimidine derivatives as Glycogen Synthase Kinase-3β inhibitors". W Proceedings: AACR Annual Meeting 2020; April 27-28, 2020 and June 22-24, 2020; Philadelphia, PA. American Association for Cancer Research, 2020. http://dx.doi.org/10.1158/1538-7445.am2020-lb-236.
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