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.
Publication types
-
Research Support, Non-U.S. Gov't
-
Research Support, U.S. Gov't, P.H.S.
MeSH terms
-
Antineoplastic Agents / chemical synthesis*
-
Antineoplastic Agents / metabolism
-
Antineoplastic Agents / pharmacology
-
Bryostatins
-
Drug Screening Assays, Antitumor
-
Humans
-
Lactones / chemical synthesis*
-
Lactones / metabolism
-
Lactones / pharmacology
-
Macrolides
-
Protein Kinase C / metabolism
-
Tumor Cells, Cultured
Substances
-
Antineoplastic Agents
-
Bryostatins
-
Lactones
-
Macrolides
-
bryostatin 1
-
Protein Kinase C