The Practical Synthesis of a Novel and Highly Potent Analogue of Bryostatin
Journal of the American Chemical Society2002Vol. 124(46), pp. 13648–13649
Citations Over TimeTop 10% of 2002 papers
Paul A. Wender, Jeremy L. Baryza, Chad Bennett, F. Christopher Bi, Stacey E. Brenner, Michael O. Clarke, Joshua C. Horan, Cindy Kan, Emmanuel Lacôte, Blaise Lippa, Peter G. Nell, T.M. Turner
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 cancer.
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