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Letters in Drug Design & Discovery

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

DOI: 10.2174/157018008785777324

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

Page: [369 - 376] Pages: 8

  • * (Excluding Mailing and Handling)

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