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Updated: May 14, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and evaluation as potential anticancer agents of novel tetracyclic indenoquinoline derivatives
Shubhashis Chakrabarty1, Michael S Croft, Melissa G Marko
1Department of Chemistry & Biochemistry, University of the Sciences in Philadelphia, 600 South Forty-Third Street, Philadelphia, PA 19104, USA.
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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