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

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

Author information

  • 1Department 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.

PMID:
12431074
[PubMed - indexed for MEDLINE]
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