PMID: 11311062Apr 20, 2001Paper

Novel seco cyclopropa[c]pyrrolo[3,2-e]indole bisalkylators bearing a 3,3'-arylenebisacryloyl group as a linker

Journal of Medicinal Chemistry
Y FukudaS Terashima

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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Jan 5, 1999·Bioorganic & Medicinal Chemistry Letters·Y FukudaS Terashima

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Citations

Jul 8, 2011·Photochemical & Photobiological Sciences : Official Journal of the European Photochemistry Association and the European Society for Photobiology·Marilene S OliveiraPaolo Di Mascio
Jan 6, 2007·Organic & Biomolecular Chemistry·Daniela VergaMauro Freccero
May 16, 2003·Journal of Medicinal Chemistry·Moana TercelWilliam A Denny

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