The Practical Synthesis of a Novel and Highly Potent Analogue of Bryostatin

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...

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Bibliographic Details
Published in:Journal of the American Chemical Society 2002-11, Vol.124 (46), p.13648-13649
Main 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
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - metabolism
Antineoplastic Agents - pharmacology
Biological and medical sciences
Bryostatins
Chemistry
Drug Screening Assays, Antitumor
Exact sciences and technology
General aspects
Heterocyclic compounds
Heterocyclic compounds with o, s, se, te hetero atom and condensed derivatives
Humans
Lactones - chemical synthesis
Lactones - metabolism
Lactones - pharmacology
Macrolides
Medical sciences
Organic chemistry
Pharmacology. Drug treatments
Preparations and properties
Protein Kinase C - metabolism
Tumor Cells, Cultured
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Summary: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.
ISSN:0002-7863
1520-5126
DOI:10.1021/ja027509+