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Guest musicians: Heather Lingle and Mark Hayden

Synthesis and SAR of C12-C13-oxazoline derivatives of epothilone A

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.

Gute Arbeit gibt herrlichen Lohn, in einer Predigt über das Evangelium am Sonntage Septuagesimae, Math. XX. 1. - 16. in der Kirche St. Leonhard in Stutgard, 1738 : mit einer eingeflossenen Anweisung, wie die vorsehende Execution des verurtheilten Juden, Joseph Süß Oppenheimers, christlich anzusehen und zu gebrauchen seye, ...

von Georg Cunrad Rieger

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