The practical synthesis of a novel and highly potent analogue of bryostatin

…, MO Clarke, JC Horan, C Kan, E Lacôte…

Index: Wender, Paul A.; Baryza, Jeremy L.; Bennett, Chad E.; Bi, F. Christopher; Brenner, Stacey E.; Clarke, Michael O.; Horan, Joshua C.; Kan, Cindy; Lacote, Emmanuel; Lippa, Blaise; Nell, Peter G.; Turner, Tim M. Journal of the American Chemical Society, 2002 , vol. 124, # 46 p. 13648 - 13649

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Citation Number: 139

Abstract

Macrocycle 1 is a new highly potent analogue of bryostatin 1, a promising anti-cancer agent currently in human clinical trials. In vitro, 1 displays picomolar affinity for PKC and exhibits over 100-fold greater potency than bryostatin 1 when tested against various human cancer cell lines. Macrocycle 1 can be generated in clinically required amounts by chemical synthesis in only 19 steps (LLS) and represents a new clinical lead for the treatment of ...