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Updated: Oct 10, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and biological evaluation of highly potent analogues of epothilones B and D
K H Altmann1, G Bold, G Caravatti
1Novartis Pharma AG, TA Oncology Research, Basel, Switzerland. karl-heinz.altmann@pharma.novartis.com
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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