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Letteratura scientifica selezionata sul tema "Bioisosteres of benzene"

Autore: Grafiati

Pubblicato: 25 gennaio 2025

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Articoli di riviste sul tema "Bioisosteres of benzene"

Mykhailiuk, Pavel K. "Saturated bioisosteres of benzene: where to go next?" Organic & Biomolecular Chemistry 17, n. 11 (2019): 2839–49. http://dx.doi.org/10.1039/c8ob02812e.

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Wei, Yunlong, Zhiqi Chen, Chen Zhu, Zhen Wu, Yaohui Xu e Xinxin Wu. "Radical Carbosulfonylation of Propellane: Synthesis of Sulfonyl β-Keto-bicyclo[1,1,1]pentanes". Synthesis 53, n. 18 (16 aprile 2021): 3325–32. http://dx.doi.org/10.1055/a-1484-1028.

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Abstract (sommario):

AbstractThe construction of multiply functionalized bicyclo[1.1.1]pentanes (BCPs) is of high synthetic value, as they are frequently harnessed as bioisosteres of 1,3-disubstituted benzene rings, alkynes, and tert-butyl groups in medicinal chemistry. Herein, we disclose a practical radical-mediated carbosulfonylation of propellane for the synthesis of sulfonyl β-keto-substituted BCPs by using vinyl sulfonates as dual-function reagent. This protocol features broad functional group tolerance and excellent atom-economy, leading to a variety of valuable difunctionalized BCP derivatives under mild photochemical conditions.

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Zhao, Jin-Xin, Yu-Xuan Chang, Chi He, Benjamin J. Burke, Michael R. Collins, Matthew Del Bel, Jeff Elleraas et al. "1,2-Difunctionalized bicyclo[1.1.1]pentanes: Long–sought-after mimetics for ortho/meta-substituted arenes". Proceedings of the National Academy of Sciences 118, n. 28 (8 luglio 2021): e2108881118. http://dx.doi.org/10.1073/pnas.2108881118.

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Abstract (sommario):

The development of a versatile platform for the synthesis of 1,2-difunctionalized bicyclo[1.1.1]pentanes to potentially mimic ortho/meta-substituted arenes is described. The syntheses of useful building blocks bearing alcohol, amine, and carboxylic acid functional handles have been achieved from a simple common intermediate. Several ortho- and meta-substituted benzene analogs, as well as simple molecular matched pairs, have also been prepared using this platform. The results of in-depth ADME (absorption, distribution, metabolism, and excretion) investigations of these systems are presented, as well as computational studies which validate the ortho- or meta-character of these bioisosteres.

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Karmacharya, Ujjwala, Diwakar Guragain, Prakash Chaudhary, Jun-Goo Jee, Jung-Ae Kim e Byeong-Seon Jeong. "Novel Pyridine Bioisostere of Cabozantinib as a Potent c-Met Kinase Inhibitor: Synthesis and Anti-Tumor Activity against Hepatocellular Carcinoma". International Journal of Molecular Sciences 22, n. 18 (7 settembre 2021): 9685. http://dx.doi.org/10.3390/ijms22189685.

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Two novel bioisosteres of cabozantinib, 3 and 4, were designed and synthesized. The benzene ring in the center of the cabozantinib structure was replaced by trimethylpyridine (3) and pyridine (4), respectively. Surprisingly, the two compounds showed extremely contrasting mesenchymal–epithelial transition factor (c-Met) inhibitory activities at 1 μM concentration (4% inhibition of 3 vs. 94% inhibition of 4). The IC50 value of compound 4 was 4.9 nM, similar to that of cabozantinib (5.4 nM). A ligand-based docking study suggested that 4 includes the preferred conformation for the binding to c-Met in the conformational ensemble, but 3 does not. The anti-proliferative activity of compound 4 against hepatocellular carcinoma (Hep3B and Huh7) and non-small-cell lung cancer (A549 and H1299) cell lines was better than that of cabozantinib, whereas 3 did not show a significant anti-proliferative activity. Moreover, the tumor selectivity of compound 4 toward hepatocellular carcinoma cell lines was higher than that of cabozantinib. In the xenograft chick tumor model, compound 4 inhibited Hep3B tumor growth to a much greater extent than cabozantinib. The present study suggests that compound 4 may be a good therapeutic candidate against hepatocellular carcinoma.

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Diepers, H. Erik, e Johannes C. L. Walker. "(Bio)isosteres of ortho- and meta-substituted benzenes". Beilstein Journal of Organic Chemistry 20 (19 aprile 2024): 859–90. http://dx.doi.org/10.3762/bjoc.20.78.

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Abstract (sommario):

Saturated bioisosteres of substituted benzenes offer opportunities to fine-tune the properties of drug candidates in development. Bioisosteres of para-benzenes, such as those based on bicyclo[1.1.1]pentane, are now very common and can be used to increase aqueous solubility and improve metabolic stability, among other benefits. Bioisosteres of ortho- and meta-benzenes were for a long time severely underdeveloped by comparison. This has begun to change in recent years, with a number of potential systems being reported that can act as bioisosteres for these important fragments. In this review, we will discuss these recent developments, summarizing the synthetic approaches to the different bioisosteres as well as the impact they have on the physiochemical and biological properties of pharmaceuticals and agrochemicals.

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Denisenko, Aleksandr, Pavel Garbuz, Svetlana V. Shishkina, Nataliya M. Voloshchuk e Pavel K. Mykhailiuk. "Saturated Bioisosteres of ortho ‐Substituted Benzenes". Angewandte Chemie 132, n. 46 (18 agosto 2020): 20696–702. http://dx.doi.org/10.1002/ange.202004183.

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Denisenko, Aleksandr, Pavel Garbuz, Svetlana V. Shishkina, Nataliya M. Voloshchuk e Pavel K. Mykhailiuk. "Saturated Bioisosteres of ortho ‐Substituted Benzenes". Angewandte Chemie International Edition 59, n. 46 (18 agosto 2020): 20515–21. http://dx.doi.org/10.1002/anie.202004183.

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Chalmers, Benjamin A., Hui Xing, Sevan Houston, Charlotte Clark, Sussan Ghassabian, Andy Kuo, Benjamin Cao et al. "Validating Eaton's Hypothesis: Cubane as a Benzene Bioisostere". Angewandte Chemie International Edition 55, n. 11 (5 febbraio 2016): 3580–85. http://dx.doi.org/10.1002/anie.201510675.

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Chalmers, Benjamin A., Hui Xing, Sevan Houston, Charlotte Clark, Sussan Ghassabian, Andy Kuo, Benjamin Cao et al. "Validating Eaton's Hypothesis: Cubane as a Benzene Bioisostere". Angewandte Chemie 128, n. 11 (5 febbraio 2016): 3644–49. http://dx.doi.org/10.1002/ange.201510675.

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Bergamaschi, Enrico, e Christopher Teskey. "Synthese im Blickpunkt: Bioisosteres of meta‐substituted benzenes". Nachrichten aus der Chemie 71, n. 3 (28 febbraio 2023): 68–71. http://dx.doi.org/10.1002/nadc.20234133609.

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Più fonti

Tesi sul tema "Bioisosteres of benzene"

Espied, Arnaud. "Approches catalytiques innovantes par des acides de Lewis pour la synthèse de composés cycliques, bicycliques et bioisostères du benzène". Electronic Thesis or Diss., université Paris-Saclay, 2024. http://www.theses.fr/2024UPASF082.

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Abstract (sommario):

Nous avons mené des recherches approfondies sur plusieurs réactions innovantes dans le domaine de la synthèse organique. Dans un premier temps, nous avons développé une réaction de cyclisation déshydratante ainsi que deux réactions en tandem, initiées par une cyclisation intramoléculaire. Ces réactions se caractérisent par leur haute diastéréosélectivité et l'utilisation d'un catalyseur à base d'un métal du groupe principal, agissant en tant qu'acide de Lewis. Cette approche nous a permis de synthétiser 27 nouveaux composés cycliques, avec des rendements pouvant atteindre 97 %. Dans un deuxième temps, nous avons mis au point une réaction tandem combinant une réaction de métathèse carbonyl-ène et un couplage déshydratant, réalisée à l'aide d'un catalyseur cationique à base de gallium sur des dérivés du benzhydrol. Cette méthode a conduit à la synthèse de 15 nouveaux composés, avec des rendements pouvant aller jusqu'à 67 %. Enfin, nous nous sommes intéressés à la réactivité des dérivés du bicyclobutane dans des cycloadditions en présence d'espèces insaturées et d'un catalyseur à base d'or. Cette approche a permis la synthèse de 5 nouveaux bioisostères du benzène, avec des rendements pouvant atteindre 90 %
We conducted extensive research on several innovative reactions in the field of organic synthesis. Initially, we developed a dehydrating cyclization reaction, as well as two tandem reactions initiated by this cyclization. These reactions are characterized by high diastereoselectivity and the use of a main-group metal-based catalyst acting as a Lewis acid. This approach allowed us to synthesize 27 new cyclic compounds with yields reaching up to 97%. Furthermore, we also developed a tandem reaction combining carbonyl-ene metathesis and a dehydrating coupling, carried out using a gallium-based cationic catalyst on benzhydrol derivatives. This method led to the synthesis of 15 new compounds, with yields of up to 67%. Finally, we investigated the reactivity of bicyclobutane derivatives in cycloadditions with unsaturated species in the presence of a gold-based catalyst. This approach enabled the synthesis of 5 new benzene bioisosteres with yields reaching up to 90%

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