SYNTHESIS AND ANTITUMOR-ACTIVITY OF NOVEL DOLASTATIN-10 ANALOGS

Authors
MIYAZAKI K KOBAYASHI M NATSUME T GONDO M MIKAMI T SAKAKIBARA K TSUKAGOSHI S
Citation
K. Miyazaki et al., SYNTHESIS AND ANTITUMOR-ACTIVITY OF NOVEL DOLASTATIN-10 ANALOGS, Chemical and Pharmaceutical Bulletin, 43(10), 1995, pp. 1706-1718
Citations number
26
Categorie Soggetti
Pharmacology & Pharmacy",Chemistry
Journal title
Chemical and Pharmaceutical Bulletin → ACNP
ISSN journal
00092363
Volume
43
Issue
10
Year of publication
1995
Pages
1706 - 1718
Database
ISI
SICI code
0009-2363(1995)43:10<1706:SAAOND>2.0.ZU;2-G
Abstract
Dolastatin 10 (1) is a potent antineoplastic pentapeptide. Novel dolas tatin 10 analogs each modified at one of the constituent amino acid de rivatives, were synthesized and their antitumor activity was evaluated against P388 leukemia in mice. The structural requirements for antitu mor activity are discussed, Some of the analogs, 31c, 35c, 38b, and 50 c showed excellent activity in vivo. Highly active 50c, which lacks th e thiazole group of 1, was selected for further development as an anti tumor agent.