179693-93-7Relevant academic research and scientific papers
Novel seco cyclopropa[c]pyrrolo[3,2-e]indole bisalkylators bearing a 3,3′-arylenebisacryloyl group as a linker
Fukuda,Seto,Furuta,Ebisu,Oomori,Terashima
, p. 1396 - 1406 (2007/10/03)
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.
Acrylamide derivatives and process for production thereof
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, (2008/06/13)
Acrylamide derivatives represented by General Formula (1) below: STR1 (One specific example of General Formula (1) is methyl (S,S)-3,3'-?3,3'-(1,4-phenylenediacryloyl)!-bis?1-chloromethyl-5-hydroxy-7-triflouromethyl-1, 2,3,6-tetrahydropyrrolo?3,2-e!indole-8-carboxylate.) The acrylamide derivatives represented by General Formula (1) is highly selective to cancer cells, less toxic, and highly active also against solid tumor.
