The practical synthesis of a novel and highly potent analogue of bryostatin |
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| Authors: | Wender Paul A Baryza Jeremy L Bennett Chad E Bi F Christopher Brenner Stacey E Clarke Michael O Horan Joshua C Kan Cindy Lacôte Emmanuel Lippa Blaise Nell Peter G Turner Tim M |
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| Institution: | Department of Chemistry, Stanford University, Stanford, California 94305-5080, USA. wenderp@stanford.edu |
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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. |
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