Synthesis and biological evaluation of highly potent analogues of epothilones B and D.

ID: ALA1132846

Journal: Bioorg Med Chem Lett

Title: Synthesis and biological evaluation of highly potent analogues of epothilones B and D.

Authors: Altmann KH, Bold G, Caravatti G, Flörsheimer A, Guagnano V, Wartmann M.

Abstract: A series of new epothilone B and D analogues incorporating fused hetero-aromatic side chains have been prepared. The synthetic strategy is based on olefin 3 as the common intermediate and allows variation of the side-chain structure in a highly convergent and stereoselective manner. Epothilone analogues 1a-d and 2a-d are more potent inhibitors of cancer cell proliferation than the corresponding parent epothilones B or D.

CiteXplore: 11133086

DOI: 10.1016/s0960-894x(00)00555-2

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