title: Synthesis and cytotoxic evaluation of a series of genistein derivatives.
abstract: Thirty genistein (= 5,7-dihydroxy-3-(4-hydroxyphenyl)-4H-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.
authors.affiliation: Institute of Functional Biomolecules, State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China.
authors.forename: Huan-Qiu
authors.initials: HQ
authors.lastname: Li
authors.forename: Hui-Ming
authors.initials: HM
authors.lastname: Ge
authors.forename: Yun-Xi
authors.initials: YX
authors.lastname: Chen
authors.forename: Chen
authors.initials: C
authors.lastname: Xu
authors.forename: Lei
authors.initials: L
authors.lastname: Shi
authors.forename: Hui
authors.initials: H
authors.lastname: Ding
authors.forename: Hai-Liang
authors.initials: HL
authors.lastname: Zhu
authors.forename: Ren-Xiang
authors.initials: RX
authors.lastname: Tan
mesh_terms: D045744:Cell Line, Tumor; D003603:Cytotoxins / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D019833:Genistein / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans
chemical_list: D003603:Cytotoxins; D019833:Genistein