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  • Title: Novel seco cyclopropa[c]pyrrolo[3,2-e]indole bisalkylators bearing a 3,3'-arylenebisacryloyl group as a linker.
    Author: Fukuda Y, Seto S, Furuta H, Ebisu H, Oomori Y, Terashima S.
    Journal: J Med Chem; 2001 Apr 26; 44(9):1396-406. PubMed ID: 11311062.
    Abstract:
    We synthesized the novel seco cyclopropa[c]pyrrolo[3,2-e]indole (CPI) bisalkylators and evaluated their antitumor activity. Among these derivatives, 11a (AT-760), in which the two seco 3-methoxycarbonyl-2-trifluoromethyl CPI (MCTFCPI) moieties are connected with a 3,3'-(1,4-phenylene)bisacryloyl group, was found to exhibit more potent cytotoxicity and antitumor activity against HeLaS3 human uterine cervix carcinoma cells and Colon 26 adenocarcinoma cells, respectively, than 8 (bizelesin, U-77,779). It also appeared that compound 11a exhibits improved in vivo efficacy in the human colon CX-1 model when compared to either compound 8 or mitomycin C (MMC). Efficacious doses for 11a were found to be 2-fold lower than those for 8.
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