Design and Synthesis of C6−C8 Bridged Epothilone A

A conformationally restrained epothilone A analogue (3) with a short bridge between methyl groups at C6 and C8 was designed and synthesized. Preliminary biological evaluation indicates 3 to be only weakly active (IC50 = 8.5 μM) against the A2780 human ovarian cancer cell line.

Saved in:
Bibliographic Details
Published inOrganic letters Vol. 10; no. 8; pp. 1565 - 1568
Main Authors Zhan, Weiqiang, Jiang, Yi, Brodie, Peggy J, Kingston, David G. I, Liotta, Dennis C, Snyder, James P
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 17.04.2008
Amer Chemical Soc
Subjects
Cell Line, Tumor
Chemistry
Chemistry, Organic
Drug Screening Assays, Antitumor
Epothilones - chemical synthesis
Epothilones - pharmacology
Female
Humans
Models, Molecular
Physical Sciences
Science & Technology
MICROTUBULE-STABILIZING AGENTS
RESISTANT
CHEMICAL BIOLOGY
HOMOALLYLIC ALCOHOLS
CHIRAL SYNTHESIS
CONFORMATION
ANTITUMOR-ACTIVITY
LEAD STRUCTURES
TUBULIN
PACLITAXEL
Online AccessGet full text

Cover

More Information
Summary:A conformationally restrained epothilone A analogue (3) with a short bridge between methyl groups at C6 and C8 was designed and synthesized. Preliminary biological evaluation indicates 3 to be only weakly active (IC50 = 8.5 μM) against the A2780 human ovarian cancer cell line.
Bibliography:Medline
NIH RePORTER
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:1523-7060
1523-7052
DOI:10.1021/ol800422q