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

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• 作者：Paul A. Wender ; Yu Nakagawa ; Katherine E. Near ; Daryl Staveness
• 刊名：Organic Letters
• 出版年：2014
• 出版时间：October 3, 2014
• 年：2014
• 卷：16
• 期：19
• 页码：5136-5139
• 全文大小：300K
• ISSN：1523-7052

文摘

Bryostatin 1 is in clinical trials for the treatment of cancer and Alzheimer鈥檚 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).