Antineoplastic agents. 465. Structural modification of resveratrol: Sodium resverastatin phosphate
Antineoplastic agents. 465. Structural modification of resveratrol: Sodium resverastatin phosphate
复制标题
DOI：
10.1021/jm010119y
复制
发表时间：
2002-06-06
影响因子：
7.3
通讯作者：
Schmidt, JM
中科院分区：
文献类型：
--
作者：
Pettit, GR;Grealish, MP;Schmidt, JM
作为白藜芦醇(1)、phenstatin （2c）和抗癌血管生成药物combretastatin A-4磷酸钠（2b）的结构/活性研究的延伸，一些相关的二苯乙烯类（14）和二苯甲酮类（16）进行了合成。(Z)-白藜芦醇（4a）的三甲基醚衍生物对人癌细胞的抑制作用最强（GI(50) = 0.01 ~ 0.001杯子/mL）。将单去甲基化衍生物（14c）转化为前药14n（白藜伐他汀磷酸钠）以进行进一步的生物学评价。并对所选化合物的抗微管蛋白和抗菌活性进行了评价。
As an extension of structure/activity investigations of resveratrol (1), phenstatin (2c), and the cancer antiangiogenesis drug sodium combretastatin A-4 phosphate (2b), syntheses of certain related stilbenes (14) and benzophenones (16) were undertaken. The trimethyl ether derivative of (Z)-resveratrol (4a) exhibited the strongest activity (GI(50) = 0.01-0.001 mug/mL) against a minipanel of human cancer cell lines. A monodemethylated derivative (14c) was converted to prodrug 14n (sodium resverastatin phosphate) for further biological evaluation. The antitubulin and antimicrobial activities of selected compounds were also evaluated.