Synthesis and in vitro anti-HSV-1 activity of a novel Hsp90 inhibitor BJ-B11.

Bioorganic & Medicinal Chemistry Letters(2011)

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摘要
In this study, a novel Hsp90 inhibitor BJ-B11, was synthesized and evaluated for in vitro antiviral activity against several viruses. Possible anti-HSV-1 mechanisms were also investigated. BJ-B11 displayed no antiviral activity against coxsackievirus B3 (CVB3), human respiratory syncytial virus (RSV) and influenza virus (H1N1), but exhibited potent anti-HSV-1 and HSV-2 activity with EC50 values of 0.42±0.18μM and 0.60±0.21μM, respectively. Additionally, the inhibitory effects of BJ-B11 against HSV-1 were likely to be introduced at early stage of infection. Our results indicate that BJ-B11 with alternative mechanisms of action is potent as an anti-HSV clinical trial candidate.
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关键词
Hsp90,MTT,Vero,MOI,PFU
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