Allosteric inhibitors of hepatitis C virus NS5B polymerase thumb domain site II: Structure-based design and synthesis of new templates
作者： Savina Malancona , Monica Donghi , Marco Ferrara , Josè I. Martin Hernando , Marco Pompei
DOI: 10.1016/J.BMC.2010.03.024
关键词:
摘要: Chronic hepatitis C virus (HCV) infections are a significant medical problem worldwide. The NS5B Polymerase of HCV plays central role in replication and is prime target for the discovery new treatment options. We recently disclosed 1H-benzo[de]isoquinoline-1,3(2H)-diones as allosteric inhibitors Polymerase. Structural SAR information guided us modification core structure leading to templates with improved activity toxicity/activity window.
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sci-hub.se 参考文章(32)
Li Jiarong, Chen Xian, Shi Daxin, Ma Shuling, Li Qing, Zhang Qi, Tang Jianhong, A new and facile synthesis of quinazoline-2,4(1H,3H)-diones. Organic Letters. ,vol. 11, pp. 1193- 1196 ,(2009) , 10.1021/OL900093H
K. E. Reed, C. M. Rice, Overview of Hepatitis C Virus Genome Structure, Polyprotein Processing, and Protein Properties Current Topics in Microbiology and Immunology. ,vol. 242, pp. 55- 84 ,(2000) , 10.1007/978-3-642-59605-6_4
Patricia C. Weber, Charles A. Lesburg, Michael B. Cable, Eric Ferrari, Zhi Hong, Anthony F. Mannarino, Crystal structure of the RNA-dependent RNA polymerase from hepatitis C virus reveals a fully encircled active site Nature Structural & Molecular Biology. ,vol. 6, pp. 937- 943 ,(1999) , 10.1038/13305
S. Bressanelli, L. Tomei, A. Roussel, I. Incitti, R. L. Vitale, M. Mathieu, R. De Francesco, F. A. Rey, Crystal structure of the RNA-dependent RNA polymerase of hepatitis C virus. Proceedings of the National Academy of Sciences of the United States of America. ,vol. 96, pp. 13034- 13039 ,(1999) , 10.1073/PNAS.96.23.13034
Gordon W Rewcastle, Graham J Atwell, Li Zhuang, Bruce C Baguley, William A Denny, None, Potential antitumor agents. 61. Structure-activity relationships for in vivo colon 38 activity among disubstituted 9-oxo-9H-xanthene-4-acetic acids. Journal of Medicinal Chemistry. ,vol. 34, pp. 217- 222 ,(1991) , 10.1021/JM00105A034
Lucjan Strekowski, Beth Wilson, Noncovalent interactions with DNA: an overview. Mutation Research. ,vol. 623, pp. 3- 13 ,(2007) , 10.1016/J.MRFMMM.2007.03.008
Lynnette R Ferguson, William A Denny, None, Genotoxicity of non-covalent interactions: DNA intercalators. Mutation Research. ,vol. 623, pp. 14- 23 ,(2007) , 10.1016/J.MRFMMM.2007.03.014
Q. Choo, G Kuo, A. Weiner, L. Overby, D. Bradley, M Houghton, Isolation of a cDNA clone derived from a blood-borne non-A, non-B viral hepatitis genome Science. ,vol. 244, pp. 359- 362 ,(1989) , 10.1126/SCIENCE.2523562
Johan Neyts, Erik De Clercq, Raghunath Singha, Yung Hsiung Chang, Asish R. Das, Subhasish K. Chakraborty, Shih Ching Hong, Shwu-Chen Tsay, Ming-Hua Hsu, Jih Ru Hwu, Structure-activity relationship of new anti-hepatitis C virus agents: heterobicycle-coumarin conjugates. Journal of Medicinal Chemistry. ,vol. 52, pp. 1486- 1490 ,(2009) , 10.1021/JM801240D
Jordan J. Feld, Jay H. Hoofnagle, Mechanism of action of interferon and ribavirin in treatment of hepatitis C Nature. ,vol. 436, pp. 967- 972 ,(2005) , 10.1038/NATURE04082