863578-84-1Relevant articles and documents
Syntheses and initial evaluation of a series of indolo-fused heterocyclic inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus
Zheng, Xiaofan,Hudyma, Thomas W.,Martin, Scott W.,Bergstrom, Carl,Ding, Min,He, Feng,Romine, Jeffrey,Poss, Michael A.,Kadow, John F.,Chang, Chong-Hwan,Wan, John,Witmer, Mark R.,Morin, Paul,Camac, Daniel M.,Sheriff, Steven,Beno, Brett R.,Rigat, Karen L.,Wang, Ying-Kai,Fridell, Robert,Lemm, Julie,Qiu, Dike,Liu, Mengping,Voss, Stacey,Pelosi, Lenore,Roberts, Susan B.,Gao, Min,Knipe, Jay,Gentles, Robert G.
, p. 2925 - 2929 (2011/06/26)
Herein, we present initial SAR studies on a series of bridged 2-arylindole-based NS5B inhibitors. The introduction of bridging elements between the indole N1 and the ortho-position of the 2-aryl moiety resulted in conformationally constrained heterocycles
Discovery of conformationally constrained tetracyclic compounds as potent hepatitis C virus NS5B RNA polymerase inhibitors
Ikegashira, Kazutaka,Oka, Takahiro,Hirashima, Shintaro,Noji, Satoru,Yamanaka, Hiroshi,Hara, Yoshinori,Adachi, Tsuyoshi,Tsuruha, Jun-Ichiro,Doi, Satoki,Hase, Yasunori,Noguchi, Toru,Ando, Izuru,Ogura, Naoki,Ikeda, Satoru,Hashimoto, Hiromasa
, p. 6950 - 6953 (2007/10/03)
We 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.
