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

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).

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Gu SX,Yang SQ,He QQ,Ma XD,Chen FE,Dai HF,Clercq ED,Balzarini J,Pannecouque C

doi

10.1016/j.bmc.2011.10.002

subject

Has Abstract

pub_date

2011-12-01 00:00:00

pages

7093-9

issue

23

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(11)00801-7

journal_volume

19

pub_type

杂志文章

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