The novel cyclopropapyrroloindole(CPI) bisalkylators bearing 3,3'-(1,4-phenylene)diacryloyl group as a linker.
The novel cyclopropapyrroloindole(CPI) bisalkylators were synthesized and their antitumor activity was evaluated. Among these derivatives, AT-760 (5a) in which the two 3-methoxycarbonyl-2-trifluoromethylCPI (MCTFCPI) moieties are connected with a 3,3'-(1,4-phenylene)diacryloyl group, was found to exhibit more prominent cytotoxicity and antitumor activity than U-77,779 (bizelesin) (1).
Fukuda
Y
Y
Central Research Laboratories, Kyorin Pharmaceutical Co. Ltd., Tochigi, Japan.
Seto
S
S
Furuta
H
H
Ebisu
H
H
Oomori
Y
Y
Terashima
S
S
D000230:Adenocarcinoma / Q000473:pathology; D000818:Animals; D018906:Antineoplastic Agents, Alkylating / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001597:Benzylidene Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D003110:Colonic Neoplasms / Q000473:pathology; D006367:HeLa Cells; D006801:Humans; D051379:Mice; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
C116802:AT 760; D018906:Antineoplastic Agents, Alkylating; D001597:Benzylidene Compounds; D011758:Pyrroles