Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents

M Dong, J Zhang, X Peng, H Lu, L Yun, S Jiang…

Index: Dong, Ming-Xin; Zhang, Jian; Peng, Xu-Qing; Lu, Hong; Yun, Liu-Hong; Jiang, Shibo; Dai, Qiu-Yun European Journal of Medicinal Chemistry, 2010 , vol. 45, # 9 p. 4096 - 4103

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Citation Number: 10

Abstract

By modifying the chemical structure of anti-orthopoxvirus compound ST-246, we designed and synthesized a series of tricyclononene carboxamide derivatives and tested their anti- HIV-1 activity and cytotoxicity. We found that benzoimidazol-containing compound 7g was highly effective in inhibiting HIV-1 R5 infection with an IC50 value of 0.41 μM and a selectivity index of 292, but it exhibited no significant inhibitory activity on HIV-1 reverse ...