期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 6, 页码 1641-1645出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.12.116
关键词
P21 deficient; antiproliferative; structure activity relationship; checkpoint
A novel series of antiproliferative agents containing pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides, selective for p21-deficient cells, were identified by high-throughput screening. Exploration of the SAR relationships in the headpiece, core, and tailpiece is described. Strict steric, positional, and electronic requirements were observed, with a clear preference for both core nitrogens, a thienoyl headpiece, and meta substituted tailpiece. (c) 2007 Elsevier Ltd. All rights reserved.
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