GOSSYPOL AND DERIVATIVES - A NEW CLASS OF ALDOSE REDUCTASE INHIBITORS
GOSSYPOL AND DERIVATIVES - A NEW CLASS OF ALDOSE REDUCTASE INHIBITORS
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DOI：
10.1021/jm00115a021
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发表时间：
1991-11-01
影响因子：
7.3
通讯作者：
ROYER, RE
中科院分区：
文献类型：
--
作者：
DECK, LM;VANDERJAGT, DL;ROYER, RE
棉酚及其17个衍生物被用来抑制人胎盘中的醛糖还原酶。棉酚和一些衍生物是有效的抑制剂。抑制活性的顺序被解释为与醛糖还原酶抑制剂位置的卡多-夏普莱斯药效团模型有关。该模型的结构方面而不是电子方面被发现适用于这一系列化合物。
Gossypol and 17 derivatives were tested as inhibitors of aldose reductase from human placenta. Gossypol and a number of the derivatives were potent inhibitors. The order of inhibitory activity was interpreted in relation to the Kador-Sharpless pharmacophor model for the aldose reductase inhibitor site. The structural but not the electronic aspects of the model were found to apply to this series of compounds.