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Synthesis and Cytotoxic Evaluation of a Series of Genistein Derivatives
Author(s) -
Li HuanQiu,
Ge HuiMing,
Chen YunXi,
Xu Chen,
Shi Lei,
Ding Hui,
Zhu HaiLiang,
Tan RenXiang
Publication year - 2006
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.200690049
Subject(s) - genistein , chemistry , cytotoxic t cell , in vitro , stereochemistry , cell culture , benzopyran , combinatorial chemistry , pharmacology , biochemistry , endocrinology , biology , genetics
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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