Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375028 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
The SAR of a series of new epothilone A derivatives with a 2-substituted-1,3-oxazoline moiety trans-fused to the C12–C13 bond of the deoxy macrocycle have been investigated with regard to tubulin polymerization induction and cancer cell growth inhibition. Significant differences in antiproliferative activity were observed between different analogs, depending on the nature of the substituent at the 2-position of the oxazoline ring. The most potent compounds showed comparable activity with the natural product epothilone A. Modeling studies provide a preliminary rationale for the observed SAR.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Bernhard Pfeiffer, Kurt Hauenstein, Philipp Merz, Jürg Gertsch, Karl-Heinz Altmann,