Synthesis and evaluation as potential anticancer agents of novel tetracyclic indenoquinoline derivatives.
Shubhashis Chakrabarty, Michael S Croft, Melissa G Marko, Guillermo Moyna
Department of Chemistry & Biochemistry, University of the Sciences in Philadelphia, 600 South Forty-Third Street, Philadelphia, PA 19104, USA.
Bioorganic & medicinal chemistry 2013 Mar 1We 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. Copyright © 2012 Elsevier Ltd. All rights reserved.
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Shubhashis Chakrabarty, Michael S Croft, Melissa G Marko, Guillermo Moyna. Synthesis and evaluation as potential anticancer agents of novel tetracyclic indenoquinoline derivatives. Bioorganic & medicinal chemistry. 2013 Mar 1;21(5):1143-9
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PMID: 23357037
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