Document Detail


Synthesis and biological activity of naphthyl-substituted (B-ring) benzophenone derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
MedLine Citation:
PMID:  21719299     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
A novel series of benzophenone derivatives with B-ring substituted by naphthyl ring has been synthesized and evaluated as non-nucleoside HIV-1 reverse transcriptase inhibitors. Most of these compounds showed good to moderate activity against wild-type HIV-1 and mutated viruses. In particular, the analogue 10i demonstrated the most potent activity against wild-type HIV-1 with an EC(50) value of 4.8nM, and with a high selectivity index up to 10347.9, it also proved to be active against the HIV-1 double mutant strain A(17) (K103N+Y181C) with an EC(50) value of 2.1μM. In addition, the molecular modeling study was used to explore the major interactions between the potent inhibitors with the HIV-1 RT. The investigation of the structure-activity relationships may serve as an important lead for the further optimization.
Authors:
Xiao-Dong Ma; Xuan Zhang; Hui-Fang Dai; Shi-Qiong Yang; Liu-Meng Yang; Shuang-Xi Gu; Yong-Tang Zheng; Qiu-Qin He; Fen-Er Chen
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-6-15
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  -     ISSN:  1464-3391     ISO Abbreviation:  -     Publication Date:  2011 Jun 
Date Detail:
Created Date:  2011-7-1     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Crown Copyright © 2011. Published by Elsevier Ltd. All rights reserved.
Affiliation:
Department of Chemistry, Fudan University, Shanghai 200433, PR China.
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