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

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.

SUBMITTER: Winfield LL

PROVIDER: S-EPMC4283767 | biostudies-literature | 2008

REPOSITORIES: biostudies-literature

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

Winfield Leyte L LL Smith Dayle M DM Halemano Kalani K Leggett Carmine S CS

Letters in drug design & discovery 20080101 6

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. ...[more]

PMID: 25568641

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