title: Computer-guided design, synthesis, and protein kinase C affinity of a new salicylate-based class of bryostatin analogs.
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).
authors.affiliation: Departments of Chemistry and Chemical and Systems Biology, Stanford University , Stanford, California 94305, United States.
authors.forename: Paul A
authors.initials: PA
authors.lastname: Wender
authors.forename: Yu
authors.initials: Y
authors.lastname: Nakagawa
authors.forename: Katherine E
authors.initials: KE
authors.lastname: Near
authors.forename: Daryl
authors.initials: D
authors.lastname: Staveness
mesh_terms: D054713:Bryostatins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D011493:Protein Kinase C / Q000187:drug effects*; D012459:Salicylates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D054713:Bryostatins; D012459:Salicylates; C046785:bryostatin 1; D011493:Protein Kinase C