期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 14, 期 13, 页码 3407-3410出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2004.04.081
关键词
benzopyranone; estrogen receptor modulator
Starting from a phenol screening hit (6), three series of benzopyranone selective estrogen receptor modulators (SERMs) have been designed, synthesized, and analyzed for both estrogen receptor alpha binding affinity and in vitro activity in two cell assays. The lead compound identified, SP500263 (13), was more potent than raloxifene and tamoxifen in a cell-based assay measuring inhibition of interleukin-6 release. (C) 2004 Elsevier Ltd. All rights reserved.
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