Synthesis of novel spirobibenzopyrans as potent anticancer leads inducing apoptosis in HeLa cells |
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| Institution: | 1. Environmental Chemistry Laboratory, Department of Studies in Environmental Science, University of Mysore, Manasagangothri, Mysore 570 006, Karnataka, India;2. PG Department of Chemistry, JSS College for Women, Sarswathipuram, Mysore 570 009, Karnataka, India;3. Department of Chemistry, JT College, Gadag 582 101, Karnataka, India;4. Department of Studies in Chemistry, University of Mysore, Manasagangothri, Mysore 570 006, Karnataka, India;5. FS-AQCL, CSIR-CFTRI, Mysore, India |
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| Abstract: | 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 G0/G1 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. |
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| Keywords: | Spirobibenzopyrans Anticancer activity Apoptosis inducers FACs studies Alkaline comet assay |
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