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Synthesis and antitumor evaluation of benzopsoralen analogues
Authors:Oliveira Ana M A G  Oliveira-Campos Ana M F  Rodrigues Lígia M  Raposo M Manuela M  Machado Antonio E H  Nascimento M São José  Nazareth N  Pinto Madalena
Affiliation:Centro de Química, Universidade do Minho, Campus de Gualtar, 4710-057 Braga, Portugal.
Abstract:The synthesis of five new tetracyclic benzopsoralen analogues, compounds 2-6, with 9H-xanthen-9-one or 9H-carbazole frameworks, is described. Their inhibitory effects on the growth of three human tumor cell lines (MCF-7, SF-268, and NCI-460) were evaluated, and discussed in terms of structure-activity relationship, taking into account both geometric and electronic features. Generally, the angular compounds showed significant biological activities, but the arrangement of functional groups also contributed to the overall activity.
Keywords:Antitumor activity  Tumor growth inhibition  Benzopsoralen  Structure–activity relationship (SAR)  Cytotoxic activity  Carbazoles  Xanthones
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