title: Synthesis and structure-activity relationships of 1,5-diazaanthraquinones as antitumour compounds.
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.
authors.affiliation: Departamento de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad Complutense, 28040 Madrid, Spain.
authors.forename: Carmen
authors.initials: C
authors.lastname: Avendaño
authors.forename: José María
authors.initials: JM
authors.lastname: Pérez
authors.forename: Maria del Mar
authors.initials: Mdel M
authors.lastname: Blanco
authors.forename: Jesús Angel
authors.initials: JA
authors.lastname: de la Fuente
authors.forename: Sonia
authors.initials: S
authors.lastname: Manzanaro
authors.forename: María Jesús
authors.initials: MJ
authors.lastname: Vicent
authors.forename: María Jesús
authors.initials: MJ
authors.lastname: Martín
authors.forename: Nélida
authors.initials: N
authors.lastname: Salvador-Tormo
authors.forename: J Carlos
authors.initials: JC
authors.lastname: Menéndez
mesh_terms: D000880:Anthraquinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001372:Aza Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000880:Anthraquinones; D000970:Antineoplastic Agents; D001372:Aza Compounds