Paul A Wender,
Jeremy L Baryza,
Chad E Bennett,
F Christopher Bi,
Stacey E Brenner,
Michael O Clarke,
Joshua C Horan,
Cindy Kan, Emmanuel Lacôte,
Blaise Lippa,
Peter G Nell,
Tim M Turner
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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.
Journal of the American Chemical Society 12/2002; 124(46):13648-9. · 9.91 Impact Factor
