The novel cyclopropapyrroloindole(CPI) bisalkylators bearing methoxycarbonyl and trifluoromethyl groups.
The novel 3-methoxycarbonyl-2-trifluoromethylcyclopropapyrroloindole (MCTFCPI) bisalkylators were synthesized and their antitumor activity was evaluated. Among these derivatives, 7f in which two MCTFCPI moieties are connected with a 5,5'-bis(2-carbonyl-1H-indole) group, was found to exhibit more prominent cytotoxicity and antitumor activity than U-77,779 (bizelesin) (2).
Fukuda
Y
Y
Central Research Laboratories, Kyorin Pharmaceutical Co. Ltd., Tochigi, Japan.
Furuta
H
H
Kusama
Y
Y
Ebisu
H
H
Oomori
Y
Y
Terashima
S
S
D000818:Animals; D018906:Antineoplastic Agents, Alkylating / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D000080890:Duocarmycins; D006367:HeLa Cells; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D051379:Mice; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured; D014508:Urea / Q000031:analogs & derivatives / Q000494:pharmacology
D018906:Antineoplastic Agents, Alkylating; D000080890:Duocarmycins; D007211:Indoles; D011758:Pyrroles; D014508:Urea; C072257:bizelesin