Synthesis and evaluation as potential anticancer agents of novel tetracyclic indenoquinoline derivatives

Bioorg Med Chem. 2013 Mar 1;21(5):1143-9. doi: 10.1016/j.bmc.2012.12.026.

Shubhashis Chakrabarty ¹, Michael S Croft, Melissa G Marko, Guillermo Moyna

Affiliations

Affiliation

1 Department of Chemistry & Biochemistry, University of the Sciences in Philadelphia, 600 South Forty-Third Street, Philadelphia, PA 19104, USA.

PMID: 23357037 DOI: 10.1016/j.bmc.2012.12.026

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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