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Sci. Pharm. 2012, 80(1), 29-36; https://doi.org/10.3797/scipharm.1109-09 (registering DOI)
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
Author to whom correspondence should be addressed.
Received: 17 September 2011 / Accepted: 1 November 2011 / 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.
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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.
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.
KRAUSS, Jürgen; KÖBLER, Daniela; MILLER, Verena; BRACHER, Franz. 2012. "Synthesis by Ring-Closing Metathesis and Cytotoxic Evaluation of Novel Thienylmacrolactones." Sci. Pharm. 80, no. 1: 29-36.
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