A preliminary assessment of the structure-activity relationship of benzimidazole-based anti-proliferative agents

被引：7

作者：

Winfield, Leyte L. ^{[1
]}

Smith, Dayle M. ^{[2
]}

Halemano, Kalani ^{[2
]}

Leggett, Carmine S. ^{[1
]}

机构：

[1] Spelman Coll, Dept Chem, Atlanta, GA 30314 USA

[2] Whitman Coll, Dept Phys, Atlanta, GA 30314 USA

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2008年 / 5卷 / 06期

关键词：

3D pharmacophore; benzimidazole; PDK1; prostate cancer; SAR; anti-proliferative;

D O I：

10.2174/157018008785777324

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

PDK1 is pivotal in the development and progression of several cancers. A 3D pharmacophore was developed for pyrazole derivatives displaying anti-proliferative activity and PDK1 inhibition. The pharmacophore was utilized in the design of benzimidazole analogs. Our preliminary results indicate the pharmacophore should be useful in designing PDK1 inhibitors and anti-proliferative agents.

引用

页码：369 / 376

页数：8

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