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    Bioorg Med Chem. 2009 Sep 15;17(18):6715-27. Epub 2009 Jul 25.

    Synthesis and structure-activity relationships of N-aryl(indol-3-yl)glyoxamides as antitumor agents.

    Marchand P, Antoine M, Le Baut G, Czech M, Baasner S, Günther E.

    Source

    Nantes Université, Nantes Atlantique Universités, Département de Pharmacochimie, IICiMed UPRES EA 1155, Faculté de Pharmacie, 1 rue Gaston Veil 44035 Nantes, France. pascal.marchand@univ-nantes.fr

    Abstract

    The synthesis and study of the structure-activity relationships of cytotoxic compounds based on N-pyridinyl or N-aryl-2-(1-benzylindol-3-yl)glyoxamide skeleton, represented by the lead structures D-24241 and D-24851, are described. The presence of N-(pyridin-4-yl) moiety was crucial for activity and 2-[1-(4-chloro-3-nitrobenzyl)-1H-indol-3-yl]-2-oxo-N-(pyridin-4-yl)acetamide (55), the most potent derivative, showed IC(50)=39 nM, 51 nM and 11 nM against HeLa/KB (human cervix carcinoma), L1210 (murine leukemia) and SKOV3 (human ovarian carcinoma) cell lines proliferation assay, respectively, as active as the lead compounds.

    PMID:
    19682911
    [PubMed - indexed for MEDLINE]

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