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 microM) against the A2780 human ovarian cancer cell line.
Zhan
Weiqiang
W
Department of Chemistry, Emory University, Atlanta, GA 30322, USA.
Jiang
Yi
Y
Brodie
Peggy J
PJ
Kingston
David G I
DG
Liotta
Dennis C
DC
Snyder
James P
JP
D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D034261:Epothilones / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D006801:Humans; D008958:Models, Molecular
D034261:Epothilones; C093787:epothilone A