Synthesis and structure-activity relationships of 1,5-diazaanthraquinones as antitumour compounds.
Avendaño C, Pérez JM, Blanco Mdel M, de la Fuente JA, Manzanaro S, Vicent MJ, Martín MJ, Salvador-Tormo N, Menéndez JC.
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.