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Bioorg Med Chem. 2012 Oct 1;20(19):5745-56. doi: 10.1016/j.bmc.2012.08.005. Epub 2012 Aug 16.

Design, synthesis, and biological evaluation of the analogues of glaziovianin A, a potent antitumor isoflavone.

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  • 1Department of Chemistry, Graduate School of Pure and Applied Sciences, University of Tsukuba, Tennodai, Tsukuba 305-8571, Japan. hayakawa@chem.tsukuba.ac.jp

Abstract

Various analogues of glaziovianin A, an antitumor isoflavone, were synthesized, and their biological activities were evaluated. O(7)-modified glaziovianin A showed strong cytotoxicity against HeLa S(3) cells. Compared to glaziovianin A, the O(7)-benzyl and O(7)-propargyl analogues were more cytotoxic against HeLa S(3) cells and more potent M-phase inhibitors. Furthermore, O(7)-modified molecular probes of glaziovianin A were synthesized for biological studies.

Copyright © 2012 Elsevier Ltd. All rights reserved.

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