Abstract

The ~ first members of a new class of designed bryostatin analogues are synthesized using a novel, convergent macmtransacetalization strategy. These simplified analogues, lacking the A-ring of bryostatin I and possessing a simplified B-ring, exhibit significant protein kinase C binding affinities and growth inhibitory activities against several human cancer cell lines. © 1998 Elsevier Science Ltd. All rights reserved. The bryostatins are a family of 20 macrocyclic lactones isolated from marine bryozoa and found to exhibit promising cancer chemotherapeutic activity.t'2 Bryostatin 1 is currently in expanded phase II human clinical trials for the treatment of various types of cancer) M eO2 H Q \ / H ~ o A c

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