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Synthesis and Cytotoxic Evaluation of a Series of Genistein Derivatives

✍ Scribed by Huan-Qiu Li; Hui-Ming Ge; Yun-Xi Chen; Chen Xu; Lei Shi; Hui Ding; Hai-Liang Zhu; Ren-Xiang Tan

Publisher
John Wiley and Sons
Year
2006
Tongue
English
Weight
124 KB
Volume
3
Category
Article
ISSN
1612-1872

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✦ Synopsis

Abstract

Thirty genistein (=5,7‐dihydroxy‐3‐(4‐hydroxyphenyl)‐4__H__‐1‐benzopyran‐4‐one; GEN) derivatives were synthesized from genistein through a facile approach in high yields. Compounds 9, 11, 12, 23–30 were reported for the first time, while 13–22 have already been reported in our recent paper. The cytotoxic activities of these compounds were evaluated against a human nasopharyngeal epidermoid tumor cell line KB. Compounds 7–9, 12, 14, 16–19, 21, 24, 27, 29 showed remarkable antitumor activities in vitro, which was comparable with 5‐fluorouracil, an anticancer drug. On the basis of the obtained experimental data, structure–effect relationships were discussed.

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