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
Letters in Drug Design & Discovery
Title: A Preliminary Assessment of the Structure-Activity Relationship of Benzimidazole-Based Anti-Proliferative Agents
Volume: 5 Issue: 6
Author(s): Leyte L. Winfield, Dayle M. Smith, Kalani Halemano and Carmine S. Leggett
Affiliation:
Keywords: 3D Pharmacophore, Benzimidazole, PDK1, Prostate cancer, SAR, Anti-proliferative
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.
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Winfield L. Leyte, Smith M. Dayle, Halemano Kalani and Leggett S. Carmine, A Preliminary Assessment of the Structure-Activity Relationship of Benzimidazole-Based Anti-Proliferative Agents, Letters in Drug Design & Discovery 2008; 5 (6) . https://dx.doi.org/10.2174/157018008785777324
DOI https://dx.doi.org/10.2174/157018008785777324 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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