SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY OF A CYCLIC ANALOG OF DOLASTATIN-10

Authors
PONCET J HORTALA L BUSQUET M GUERITTEVOEGELEIN F THORET S PIERRE A ATASSI G JOUIN P
Citation
J. Poncet et al., SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY OF A CYCLIC ANALOG OF DOLASTATIN-10, Bioorganic & medicinal chemistry letters, 8(20), 1998, pp. 2855-2858
Citations number
18
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
20
Year of publication
1998
Pages
2855 - 2858
Database
ISI
SICI code
0960-894X(1998)8:20<2855:SAAAOA>2.0.ZU;2-R
Abstract
A cyclic analog of the natural antiproliferative compound dolastatin 1 0 was synthesized by introducing an ester link between the N- and C-te rminal residues which were modified accordingly. The final macrolacton ization was performed by using isopropenyl chloroformate and DMAP as r eagents. This analog exhibits submicromolar antiproliferative activity against the L1210 and HT29 cell lines and inhibits in vitro tubulin p olymerization (IC50, 39 mu M). (C) 1998 Elsevier Science Ltd. All ligh ts reserved.