Design and synthesis of novel benzimidazole derivatives as inhibitors of hepatitis B virus |
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| Authors: | Yu Luo Jia-Ping Yao Li Yang Chun-Lan Feng Wei Tang Gui-Feng Wang Jian-Pin Zuo Wei Lu |
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| Institution: | 1. Department of Chemistry, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, PR China;2. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, 555 Zu Chongzhi Road, Shanghai 201203, PR China |
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| Abstract: | A series of novel benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. The preliminary SAR was discussed. Compound 12a, with IC50 <0.41 μM and SI >81.2, was the most promising compound and selected as the benchmark compound for further optimization. |
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