期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 18, 期 14, 页码 5039-5047出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.05.081
关键词
HIV-1; Reverse transcriptase; NNRTIs; DABPs; Molecular hybridization; SAR
资金
- National Natural Science Foundation of China [20872018, 30672536]
- Concerted Actions of the K.U. Leuven [GOA-10/14]
- European Commission
Molecular hybridization of the known anti-HIV-1 template DPC083 and etravirine based on docking model overlay has been generated a novel series of diarylbenzopyrimidine analogues (DABPs) (5a-z). These new hybrids were assessed for their activity against HIV in MT-4 cell cultures. Most of these compounds showed good activity against wild-type HIV-1 and mutant viruses. In particular, compound 5r showed the most potent activity against wild-type HIV-1 with an EC50 value of 1.8 nM, and with a selectivity index up to 111,954. It also proved more active against mutant L100I, K103N, Y188L, and K103N + Y181C RT HIV-1 strains than efavirenz. (C) 2010 Elsevier Ltd. All rights reserved.
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