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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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
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Accepted: 1 November 2011
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Published: 1 November 2011
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
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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 StyleKRAUSS, 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
