J Am Chem Soc. 2002 Nov 20;124(46):13648-9.

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

Wender PA, Baryza JL, Bennett CE, Bi FC, Brenner SE, Clarke MO, Horan JC, Kan C, Lacôte E, Lippa B, Nell PG, Turner TM.

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Department of Chemistry, Stanford University, Stanford, California 94305-5080, USA. wenderp@stanford.edu

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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The practical synthesis of a novel and highly potent analogue of bryostatin.
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J Am Chem Soc. 2002 Nov 20 ;124(46):13648-9.

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