title: Synthesis by ring-closing metathesis and cytotoxic evaluation of novel thienylmacrolactones.
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.
authors.affiliation: Department of Pharmacy - Center for Drug Research, Ludwig-Maximilians University, Butenandtstr. 5-13, 81377 Munich, Germany.
authors.forename: Jürgen
authors.initials: J
authors.lastname: Krauss
authors.forename: Daniela
authors.initials: D
authors.lastname: Köbler
authors.forename: Verena
authors.initials: V
authors.lastname: Miller
authors.forename: Franz
authors.initials: F
authors.lastname: Bracher