Synthesis of novel spirobibenzopyrans as potent anticancer leads inducing apoptosis in HeLa cells

Kar, Swayamsiddha and Ramamoorthy, Gayathri and Mitra, Kartik and Naveen, S. and Mahesha and Mavileti, Sai Kiran and Lokanath, N. K. and Doble, Mukesh and Golakoti, Nageswara Rao (2020) Synthesis of novel spirobibenzopyrans as potent anticancer leads inducing apoptosis in HeLa cells. Bioorganic & Medicinal Chemistry Letters, 30 (12). ISSN 1464-3405

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Spirobibenzopyrans are an unexplored class of therapeutics. We report the anticancer activity of novel spirobibenzopyrans, synthesized by a one-pot reaction and extensively characterized. Structure of one of the spirobibenzopyran has been determined by the single crystal XRD technique. The in vitro anticancer activity of these derivatives across the NCI 60-cell line panel was evaluated and for the first time their mechanism of action against HeLa cells was probed via cell morphology analysis and cell cycle analysis. They were determined to be apoptosis inducers with cell cycle arrest in G(0)/G(1) and S phase suggesting CDK-4 protein inhibition and the inhibition of DNA replication. The DNA inhibition was studied and confirmed using the alkaline comet assay for the compound CHX-4MO-SAL showing S phase inhibition. Further, conformity with the in silico Lipinski's score signify the potential of spirobibenzopyrans as anticancer leads.

Item Type: Article
Uncontrolled Keywords: Spirobibenzopyrans; Anticancer activity; Apoptosis inducers; FACs studies; Alkaline comet assay
Subjects: D Physical Science > Physics
Divisions: Department of > Physics
Depositing User: Mr Umendra uom
Date Deposited: 01 Apr 2021 10:23
Last Modified: 05 Jul 2022 07:26

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