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

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

  • Bioorg Med Chem. 2009 Sep 15;17(18):6715-27. doi: 10.1016/j.bmc.2009.07.048.
Pascal Marchand 1,  Maud Antoine,  Guillaume Le Baut,  Michael Czech,  Silke Baasner,  Eckhard Günther
Affiliations

Affiliation

  • 1 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
PMID: 19682911 DOI: 10.1016/j.bmc.2009.07.048
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.

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