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Synthesis, antitumor evaluation, and apoptosis-inducing activity of hydroxylated (E)-stilbenes.

作者信息

Lion Cedric J, Matthews Charles S, Stevens Malcolm F G, Westwell Andrew D

机构信息

Cancer Research U.K. Experimental Cancer Chemotherapy Research Group, Centre for Biomolecular Sciences, School of Pharmacy, University of Nottingham, UK.

出版信息

J Med Chem. 2005 Feb 24;48(4):1292-5. doi: 10.1021/jm049238e.

DOI:10.1021/jm049238e
PMID:15715501
Abstract

The parallel solution-phase synthesis of a series of 30 monohydroxylated (E)-stilbene analogues is described. In vitro screening revealed low micromolar activity (GI(50)) against the MDA MB 468 breast cancer cell line. Activity in MDA MB 468 cells correlated with the ability to induce apoptosis following drug treatment by the most potent agents in the series, e.g., 5dy and 5jy, an observation further reinforced by AnnexinV-FITC analysis and fluorescence microscopy.

摘要

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