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Volume 80
Issue 1
10.3797/scipharm.1109-09
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Article

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

by
Jürgen KRAUSS
*,
Daniela KÖBLER
,
Verena MILLER
and
Franz BRACHER
Department of Pharmacy – Center for Drug Research, Ludwig-Maximilians University, Butenandtstr. 5–13, 81377 Munich, Germany
*
Author to whom correspondence should be addressed.
Sci. Pharm. 2012, 80(1), 29-36; https://doi.org/10.3797/scipharm.1109-09
Submission received: 17 September 2011 / Accepted: 1 November 2011 / Published: 1 November 2011
Versions Notes

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

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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. https://doi.org/10.3797/scipharm.1109-09

AMA Style

KRAUSS J, KÖBLER D, MILLER V, BRACHER F. Synthesis by Ring-Closing Metathesis and Cytotoxic Evaluation of Novel Thienylmacrolactones. Scientia Pharmaceutica. 2012; 80(1):29-36. https://doi.org/10.3797/scipharm.1109-09

Chicago/Turabian Style

KRAUSS, Jürgen, Daniela KÖBLER, Verena MILLER, and Franz BRACHER. 2012. "Synthesis by Ring-Closing Metathesis and Cytotoxic Evaluation of Novel Thienylmacrolactones" Scientia Pharmaceutica 80, no. 1: 29-36. https://doi.org/10.3797/scipharm.1109-09

APA Style

KRAUSS, J., KÖBLER, D., MILLER, V., & BRACHER, F. (2012). Synthesis by Ring-Closing Metathesis and Cytotoxic Evaluation of Novel Thienylmacrolactones. Scientia Pharmaceutica, 80(1), 29-36. https://doi.org/10.3797/scipharm.1109-09

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