Computer-aided rational drug design: A novel agent (SR13668) designed to mimic the unique anticancer mechanisms of dietary indole-3-carbinol to block akt signaling

被引：130

作者：

Chao, Wan-Ru ^{[1
]}

Yean, Dawn ^{[1
]}

Amin, Khalid ^{[1
]}

Green, Carol ^{[1
]}

Jong, Ling ^{[1
]}

机构：

[1] SRI Int, Menlo Pk, CA 94025 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 50卷 / 15期

关键词：

D O I：

10.1021/jm070040e

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Indole-3-carbinol (I3C) is a naturally occurring anticancer agent and has entered clinical trials for cancer prevention. However, the clinical development of I3C has been impeded by its poor metabolic profile. The active components of I3C were used to develop a novel class of indole analogs to optimize I3C's anticancer actions, including blocking growth factor-stimulated Akt activation. The most promising of these analogs, SR13668, exhibited potent oral anticancer activity against various cancers and no significant toxicity.

引用

页码：3412 / 3415

页数：4