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

…, MJ Martı́n, N Salvador-Tormo, JC Menéndez

Index: Avendano, Carmen; Perez, Jose Maria; Blanco, Ma Del Mar; De La Fuente, Jesus Angel; Manzanaro, Sonia; Vicent, Maria Jesus; Martin, Maria Jesus; Salvador-Tormo, Nelida; Menendez, J. Carlos Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 15 p. 3929 - 3932

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Citation Number: 10

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 IC50 values in the 10− 8M range for human lung carcinoma and human melanoma, which makes them attractive candidates ...