2. Academic Validation
  3. Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs

Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs

  • Bioorg Med Chem. 2011 Dec 1;19(23):7093-9. doi: 10.1016/j.bmc.2011.10.002.
Shuang-Xi Gu 1,  Shi-Qiong Yang,  Qiu-Qin He,  Xiao-Dong Ma,  Fen-Er Chen,  Hui-Fang Dai,  Erik De Clercq,  Jan Balzarini,  Christophe Pannecouque
Affiliations

Affiliation

  • 1 Department of Chemistry, Fudan University, Shanghai 200433, People's Republic of China.
PMID: 22037050 DOI: 10.1016/j.bmc.2011.10.002
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 0.055 μM 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).

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