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

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• 作者：Ichiro Hayakawa ; Akiyuki Ikedo ; Takumi Chinen ; Takeo Usui ; Hideo Kigoshi
• 关键词：Structure&ndash ; activity relationship study ; Glaziovianin A ; Isoflavone ; Antitumor activity ; Molecular probes
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2012
• 出版时间：1 October, 2012
• 年：2012
• 卷：20
• 期：19
• 页码：5745-5756
• 全文大小：836 K

文摘

Various analogues of glaziovianin A, an antitumor isoflavone, were synthesized, and their biological activities were evaluated. O⁷-modified glaziovianin A showed strong cytotoxicity against HeLa S₃ cells. Compared to glaziovianin A, the O⁷-benzyl and O⁷-propargyl analogues were more cytotoxic against HeLa S₃ cells and more potent M-phase inhibitors. Furthermore, O⁷-modified molecular probes of glaziovianin A were synthesized for biological studies.