Efficient Solid-Phase Synthesis of FK228 Analogues as Potent Antitumoral Agents

被引：27

作者：

Di Maro, Salvatore ^{[1
]}

Pong, Rey-Chen ^{[2
]}

Hsieh, Jer-Tsong ^{[2
]}

Ahn, Jung-Mo ^{[1
]}

机构：

[1] Univ Texas Dallas, Dept Chem, Richardson, TX 75080 USA

[2] Univ Texas SW Med Ctr Dallas, Dept Urol, Dallas, TX 75390 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 21期

关键词：

D O I：

10.1021/jm800959f

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel structural analogues of a HDAC inhibitor FK228 have been synthesized by modifying the most synthetically challenging unit, (3S,4E)-3-hydroxy-7-mercaptoheptenoic acid, with simple isosteric substitutions. These changes did not alter the backbone structure from FK228 but enabled facile and rapid synthesis by using readily available starting materials and high-yielding reactions. FK228 analogues were examined for their antitumoral activity on a variety of human cancer cells and led to the identification of new potent compound.

引用

页码：6639 / 6641

页数：3

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