期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 1, 页码 718-722出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.10.039
关键词
Aromatase inhibition; Anticancer compounds; Aldol reaction; Triazoles
资金
- NSERC
- McMaster University
The discovery of a novel five-component 1,2,3-triazole-containing pharmacophore that exhibits potent and selective inhibition of aromatase (CYP 450 19A1) is described. All compounds are derived from an initial aldol reaction of a phenylacetate derivative with an aromatic aldehyde. Structure-activity data generated from both syn- and anti-aldol adducts provides initial insights into the requirements for both potency and selectivity. (C) 2011 Elsevier Ltd. All rights reserved.
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