Computer-Guided Design, Synthesis, and Protein Kinase C Affinity of a New Salicylate-Based Class of Bryostatin Analogs | Zendy

Paul A. Wender | Zendy; Yu Nakagawa | Zendy; Katherine E. Near | Zendy; Daryl Staveness | Zendy

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Computer-Guided Design, Synthesis, and Protein Kinase C Affinity of a New Salicylate-Based Class of Bryostatin Analogs

Author(s) -

Paul A. Wender,

Yu Nakagawa,

Katherine E. Near,

Daryl Staveness

Publication year - 2014

Publication title -

organic letters

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.94

H-Index - 239

eISSN - 1523-7060

pISSN - 1523-7052

DOI - 10.1021/ol502491f

Subject(s) - bryostatin 1 , protein kinase a , chemistry , protein subunit , protein kinase c , kinase , function (biology) , combinatorial chemistry , biochemistry , microbiology and biotechnology , biology , gene

Bryostatin 1 is in clinical trials for the treatment of cancer and Alzheimer's disease and is a candidate for a first-in-class approach to HIV/AIDS eradication. It is neither readily available nor optimally suited for clinical use. Using a function oriented synthesis strategy, a new class of bryostatin-inspired analogs was designed with a simplified salicylate-derived subunit, enabling step-economical synthesis (23 total steps) of agents exhibiting bryostatin-like affinity to protein kinase C (PKC).

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