Synthesis and evaluation as potential anticancer agents of novel tetracyclic indenoquinoline derivatives |
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| Authors: | Shubhashis Chakrabarty Michael S. Croft Melissa G. Marko Guillermo Moyna |
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| Affiliation: | 1. Department of Chemistry & Biochemistry, University of the Sciences in Philadelphia, 600 South Forty-Third Street, Philadelphia, PA 19104, USA;2. Department of Biological Sciences, University of the Sciences in Philadelphia, 600 South Forty-Third Street, Philadelphia, PA 19104, USA;3. Departamento de Química del Litoral, Polo Agroalimentario y Agroindustrial, Universidad de la República, Ruta 3 Km 363, Paysandú 60000, Uruguay |
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| Abstract: | We report the synthesis and evaluation as potential anticancer agents of a series of tetracyclic indenoquinolines. The compounds, which are obtained through the photoisomerization of Diels–Alder adducts formed between purpurogallin derivatives and nitrosobenzene, have in vitro antiproliferative activities in the μM to nM range against breast (MCF-7), lung epithelial (A-549), and cervical (HeLa) adenocarcinoma cells. The cytotoxicities of several of the novel tetracycles are comparable to or better than that of camptothecin. A strong correlation between the activity of the compounds and their aromaticity and planarity was observed, suggesting a mode of action similar to that of topoisomerase poisons. |
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