4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 6, Pages 1675-1677

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.01.098

Keywords

Hsp90 inhibitor; Antivirals; Herpes simplex virus

Funding

  1. Nation '863' Program of China [2007AA02Z142]
  2. Nation '211' project
  3. National Natural Science Foundation of China [30873082, 20772013]

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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 B-3 (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 +/- 0.18 mu M and 0.60 +/- 0.21 mu M, 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. (C) 2011 Elsevier Ltd. All rights reserved.

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