Avendaño Carmen, Pérez José María, Blanco Maria del Mar, de la Fuente Jesús Angel, Manzanaro Sonia, Vicent María Jesús, Martín María Jesús, Salvador-Tormo Nélida, Menéndez J Carlos
Departamento de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad Complutense, 28040 Madrid, Spain.
Bioorg Med Chem Lett. 2004 Aug 2;14(15):3929-32. doi: 10.1016/j.bmcl.2004.05.055.
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.
采用单杂环和双杂环狄尔斯-阿尔德策略合成了1,5-二氮杂蒽醌衍生物。使用三种细胞系测定了它们的体外抗肿瘤活性。其中一些化合物，特别是那些在C-3、7位带有甲基或乙基，或在C-4位带有氯原子且在C-7位带有甲基的化合物，对人肺癌和人黑色素瘤的IC(50)值在10(-8)M范围内，这使它们成为有吸引力的进一步开发为抗癌药物的候选物。
