Synthesis and anti-hepatitis B virus activity of novel benzimidazole derivatives.
A series of novel benzimidazole derivatives was synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in vitro. Strong activity against HBV replication and low cytotoxicity were generally observed in these benzimidazoles. The most promising compounds were 12a and 12b, with similar high antiviral potency (IC50 = 0.9 and 0.7 microM, respectively) and remarkable selectivity indices (>1111 and 714, respectively). They were selected for further evaluation as novel HBV inhibitors.
Li
Yun-Fei
YF
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, 555 Zuchongzhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.
Wang
Gui-Feng
GF
He
Pei-Lan
PL
Huang
Wei-Gang
WG
Zhu
Feng-Hua
FH
Gao
He-Yong
HY
Tang
Wei
W
Luo
Yu
Y
Feng
Chun-Lan
CL
Shi
Li-Ping
LP
Ren
Yu-Dan
YD
Lu
Wei
W
Zuo
Jian-Ping
JP
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004279:DNA, Viral / Q000037:antagonists & inhibitors; D006515:Hepatitis B virus / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D013329:Structure-Activity Relationship
D000998:Antiviral Agents; D001562:Benzimidazoles; D004279:DNA, Viral