Title: Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs
Authors: Gu, Shuang-Xi ×
Yang, Shi-Qiong
Chen, Fen-Er
Dai, Hui-Fang
De Clercq, Erik
Balzarini, Jan
Pannecouque, Christophe #
Issue Date: Dec-2011
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:19 issue:23 pages:7093-7099
Abstract: A series of 18 cycloalkyl arylpyrimidines (CAPYs) were designed from lead compounds diarylpyrimidines (DAPYs), synthesized and evaluated for in vitro anti-HIV activity. Among them, the compound 1p displayed potent anti-HIV-1 activity against WT HIV-1 with an EC(50) value of 0.055μM and a selectivity index (SI) >7290. The preliminary structure-activity relationship (SAR) of this new series of compounds was also investigated, which enriched the SAR of diarylpyrimidines (DAPYs).
ISSN: 0968-0896
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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