Organic Letters 2014-10-03

Improved protein kinase C affinity through final step diversification of a simplified salicylate-derived bryostatin analog scaffold.

Paul A Wender, Daryl Staveness

Index: Org. Lett. 16(19) , 5140-3, (2014)

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Abstract

Bryostatin 1, in clinical trials or preclinical development for cancer, Alzheimer's disease, and a first-of-its-kind strategy for HIV/AIDS eradication, is neither readily available nor optimally suited for clinical use. In preceding work, we disclosed a new class of simplified bryostatin analogs designed for ease of access and tunable activity. Here we describe a final step diversification strategy that provides, in only 25 synthetic steps, simplified and tunable analogs with bryostatin-like PKC modulatory activities.