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. 2000 Dec 18;10(24):2765-8.
doi: 10.1016/s0960-894x(00)00555-2.

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

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

K H Altmann et al. Bioorg Med Chem Lett. .

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.

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