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Computer-guided design, synthesis, and protein kinase C affinity of a new salicylate-based class of bryostatin
Paul A Wender1, Yu Nakagawa, Katherine E Near
1Departments of Chemistry and Chemical and Systems Biology, Stanford University , Stanford, California 94305, United States.
Abstract:
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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