Format

Send to

Choose Destination
Org Biomol Chem. 2008 Dec 21;6(24):4542-52. doi: 10.1039/b814823f. Epub 2008 Nov 6.

Design, synthesis and biological evaluation of bridged epothilone D analogues.

Author information

1
Department of Chemistry, M/C 0212, Virginia Polytechnic Institute and State University, Blacksburg, Virginia 24061, USA. qchen06@vt.edu

Abstract

Six epothilone D analogues with a bridge between the C4-methyl and the C12-methyl carbons were prepared in an attempt to constrain epothilone D to its proposed tubulin-binding conformation. Ring-closing metathesis (RCM) was employed as the key step to build the C4-C26 bridge. In antiproliferative assays in the human ovarian cancer (A2780) and prostate cancer (PC3) cell lines, and also in tubulin assembly assay, all these compounds proved to be less active than epothilone D.

PMID:
19039362
PMCID:
PMC2790820
DOI:
10.1039/b814823f
[Indexed for MEDLINE]
Free PMC Article

Supplemental Content

Full text links

Icon for Royal Society of Chemistry Icon for PubMed Central
Loading ...
Support Center