2. Academic Validation
  3. Synthesis and biological evaluation of highly potent analogues of epothilones B and D

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

  • Bioorg Med Chem Lett. 2000 Dec 18;10(24):2765-8. doi: 10.1016/s0960-894x(00)00555-2.
K H Altmann 1,  G Bold,  G Caravatti,  A Flörsheimer,  V Guagnano,  M Wartmann
Affiliations

Affiliation

  • 1 Novartis Pharma AG, TA Oncology Research, Basel, Switzerland. karl-heinz.altmann@pharma.novartis.com
PMID: 11133086 DOI: 10.1016/s0960-894x(00)00555-2
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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