设计、合成及 Glaziovianin A 的类似物的生物评价，一种强效的抗肿瘤异黄酮。
Design, synthesis, and biological evaluation of the analogues of glaziovianin A, a potent antitumor isoflavone.
机构信息
Department of Chemistry, Graduate School of Pure and Applied Sciences, University of Tsukuba, Tennodai, Tsukuba 305-8571, Japan.
出版信息
Bioorg Med Chem. 2012 Oct 1;20(19):5745-56. doi: 10.1016/j.bmc.2012.08.005. Epub 2012 Aug 16.
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.
合成了一系列抗瘤异黄酮 glaziovianin A 的类似物，并对其生物活性进行了评价。O(7)-修饰的 glaziovianin A 对 HeLa S(3)细胞表现出很强的细胞毒性。与 glaziovianin A 相比，O(7)-苄基和 O(7)-炔丙基类似物对 HeLa S(3)细胞的细胞毒性更强，并且是更强效的 M 期抑制剂。此外，还合成了 glaziovianin A 的 O(7)-修饰分子探针用于生物学研究。
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