2dxs
Crystal structure of HCV NS5B RNA polymerase complexed with a tetracyclic inhibitorCrystal structure of HCV NS5B RNA polymerase complexed with a tetracyclic inhibitor
Structural highlights
Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMedWe report a new series of hepatitis C virus NS5B RNA polymerase inhibitors containing a conformationally constrained tetracyclic scaffold. SAR studies led to the identification of 6,7-dihydro-5H-benzo[5,6][1,4]diazepino[7,1-a]indoles (19 and 20) bearing a basic pendent group with high biochemical and cellular potencies. These compounds displayed a very small shift in cellular potency when the replicon assay was performed in the presence of human serum albumin. Discovery of conformationally constrained tetracyclic compounds as potent hepatitis C virus NS5B RNA polymerase inhibitors.,Ikegashira K, Oka T, Hirashima S, Noji S, Yamanaka H, Hara Y, Adachi T, Tsuruha J, Doi S, Hase Y, Noguchi T, Ando I, Ogura N, Ikeda S, Hashimoto H J Med Chem. 2006 Nov 30;49(24):6950-3. PMID:17125247[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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