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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

A Preliminary Assessment of the Structure-Activity Relationship of Benzimidazole-Based Anti-Proliferative Agents

Author(s): Leyte L. Winfield, Dayle M. Smith, Kalani Halemano and Carmine S. Leggett

Volume 5 , Issue 6 , 2008

Page: [369 - 376] Pages: 8

DOI: 10.2174/157018008785777324

Price: $65

Abstract

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.

Keywords: 3D Pharmacophore, Benzimidazole, PDK1, Prostate cancer, SAR, Anti-proliferative


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