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Winfield LL, Smith DM, Halemano K, et al. A Preliminary Assessment of the Structure-Activity Relationship of Benzimidazole-Based Anti-Proliferative Agents. Lett Drug Des Discov. 2008;5(6):369-376doi: 10.2174/157018008785777324#sthash.5mpkAcrR.dpuf.
Winfield, L. L., Smith, D. M., Halemano, K., & Leggett, C. S. (2008). A Preliminary Assessment of the Structure-Activity Relationship of Benzimidazole-Based Anti-Proliferative Agents. Letters in drug design & discovery, 5(6), 369-376. https://doi.org/10.2174/157018008785777324#sthash.5mpkAcrR.dpuf
Winfield, Leyte L, et al. "A Preliminary Assessment of the Structure-Activity Relationship of Benzimidazole-Based Anti-Proliferative Agents." Letters in drug design & discovery vol. 5,6 (2008): 369-376. doi: https://doi.org/10.2174/157018008785777324#sthash.5mpkAcrR.dpuf
Winfield LL, Smith DM, Halemano K, Leggett CS. A Preliminary Assessment of the Structure-Activity Relationship of Benzimidazole-Based Anti-Proliferative Agents. Lett Drug Des Discov. 2008;5(6):369-376. doi: 10.2174/157018008785777324#sthash.5mpkAcrR.dpuf. PMID: 25568641; PMCID: PMC4283767.
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Lett Drug Des Discov. 2008;5(6):369-376. doi: 10.2174/157018008785777324#sthash.5mpkAcrR.dpuf.

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

Letters in drug design & discovery

Leyte L Winfield, Dayle M Smith, Kalani Halemano, Carmine S Leggett

Affiliations

  1. Department of Chemistry, Spelman College, Atlanta, GA 30314, USA.
  2. Department of Physics, Whitman College, Walla Walla, WA 99362, USA.

PMID: 25568641 PMCID: PMC4283767 DOI: 10.2174/157018008785777324#sthash.5mpkAcrR.dpuf

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; Anti-proliferative; Benzimidazole; PDK1; Prostate cancer; SAR

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