The novel cyclopropapyrroloindole(CPI) bisalkylators bearing 3,3′-(1,4-phenylene)diacryloyl group as a linker

Abstract 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 ).