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Synthesis and antitumour activity of fluorinated 1-aza and 1,8-diazaanthraquinones
M T Ramos1, L M Díaz-Guerra, S García-Copín
1Departamento de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad Complutense, Madrid, Spain.
Abstract:
A series of 3-fluoro-1-aza- and 1,8-diazaanthraquinones, structurally related to the antitumour antibiotic diazaquinomycin A, have been prepared by Diels-Alder reactions of 2-fluoro-2-propenal N, N-dimethylhydrazone and the corresponding quinones. These compounds showed potent in vitro activity against different tumour cell lines. They also showed some selectivity towards rapid-growth tumours when compared to other non-fluorinated analogues. In contrast with diazaquinomycin A, the azaanthraquinones studied here have not shown significant activity as thymidylate synthase inhibitors. Some compounds showed a high activity as inhibitors of protein, DNA and RNA biosynthesis.