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Sci. Pharm. 2012, 80(1), 29-36; doi:10.3797/scipharm.1109-09

Synthesis by Ring-Closing Metathesis and Cytotoxic Evaluation of Novel Thienylmacrolactones

Department of Pharmacy – Center for Drug Research, Ludwig-Maximilians University, Butenandtstr. 5–13, 81377 Munich, Germany
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Received: 17 September 2011 / Accepted: 1 November 2011 / Published: 1 November 2011
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Abstract

This paper describes the synthesis and biological evaluation of macrolactones containing a thienyl substituent as simple analogues of epothilones. The compounds were prepared in a brief and efficient manner from thiophene-2-carbaldehyde using a ring-closing metathesis with Grubbs I or Grubbs II catalyst as the key step. The target lactones showed only insignificant cytotoxicity, while an intermediate simple thienyl carbinol showed very promising cytotoxicity.
Keywords: Ring-closing metathesis; Grignard reaction; Macrolactones; MTT assay; Thiophenes Ring-closing metathesis; Grignard reaction; Macrolactones; MTT assay; Thiophenes
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

KRAUSS, J.; KÖBLER, D.; MILLER, V.; BRACHER, F. Synthesis by Ring-Closing Metathesis and Cytotoxic Evaluation of Novel Thienylmacrolactones. Sci. Pharm. 2012, 80, 29-36.

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