Synthesis and structure-activity relationships of 1,5-diazaanthraquinones as antitumour compounds

  • Bioorg Med Chem Lett. 2004 Aug 2;14(15):3929-32. doi: 10.1016/j.bmcl.2004.05.055.
Carmen Avendaño  1 ,  José María Pérez ,  Maria del Mar Blanco ,  Jesús Angel de la Fuente ,  Sonia Manzanaro ,  María Jesús Vicent ,  María Jesús Martín ,  Nélida Salvador-Tormo ,  J Carlos Menéndez
Affiliations
  • 1. Departamento de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad Complutense, 28040 Madrid, Spain.
PMID: 15225700 DOI: 10.1016/j.bmcl.2004.05.055
Abstract

1,5-Diazaanthraquinone derivatives were synthesized employing single and double hetero Diels-Alder strategies. Their in vitro antitumour activity was assayed using three cell lines. Some of these compounds, specially those bearing methyl or ethyl groups at the C-3,7 positions or chloro at C-4 and methyl at C-7, showed IC(50) values in the 10(-8)M range for human lung carcinoma and human melanoma, which makes them attractive candidates for further development as Anticancer agents.