SYNTHESIS AND ANTITUMOR-ACTIVITY OF NOVEL CYCLOPROPAPYRROLOINDOLE (CPI) DERIVATIVES BEARING METHOXYCARBONYL AND TRIFLUOROMETHYL GROUPS

Authors
FUKUDA Y FURUTA H SHIGA F OOMORI Y KUSAMA Y EBISU H TERASHIMA S
Citation
Y. Fukuda et al., SYNTHESIS AND ANTITUMOR-ACTIVITY OF NOVEL CYCLOPROPAPYRROLOINDOLE (CPI) DERIVATIVES BEARING METHOXYCARBONYL AND TRIFLUOROMETHYL GROUPS, Bioorganic & medicinal chemistry letters, 7(13), 1997, pp. 1683-1688
Citations number
26
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
13
Year of publication
1997
Pages
1683 - 1688
Database
ISI
SICI code
0960-894X(1997)7:13<1683:SAAONC>2.0.ZU;2-9
Abstract
The title synthesis was achieved by employing oxidative cyclization of the enaminoester as a key step. Some of these novel ycarbonyl-2-trifl uoromethylcyclopropapyrroloindole (MCTFCPI) derivatives, dl-10c,d, (+) -10d, and (S)-21b were found to exhibit antitumor activity against mur ine leukemia and murine solid tumors more prominent than that of the k nown CPI derivatives dl-4 and the clinical trial candidates 5 and 7. ( C) 1997 Elsevier Science Ltd.