224321-69-1Relevant articles and documents
Novel cyclopropapyrroloindole derivative (AT-3510) bearing methoxycarbonyl and trifluoromethyl groups
Fukuda, Yasumichi,Furuta, Hirosuke,Kusama, Yoshie,Ebisu, Hiroyuki,Oomori, Yasuo,Terashima, Shiro
, p. 1448 - 1458 (2007/10/03)
The seco-Cl 3-methoxycarbonyl-2-trifluoromethylcyclopropapyrroloindole (MCTFCPI) derivatives dl- and/or (S)-10 carrying various acyl moleties at the N6-position were synthesized along with their prodrugs (S)-12, and their antitumor activity was evaluated. Among these derivatives, AT-3510 [(S)- 12m], the novel prodrug MCTFCPI derivative carrying a 5-(7- methoxybenzofuran-2-ylcarbonyl)aminoindole-2-carbonyl group at the N6- position, was found to exhibit more excellent antitumor activity against human tumor xenografts than the clinical trial candidates carzelesin (6) and KW-2189 (7) and cisplatin.
