Synthesis and anticancer potential of benzothiazole linked phenylpyridopyrimidinones and their diones as mitochondrial apoptotic inducers

Bioorganic & Medicinal Chemistry Letters
Ahmed KamalV Lakshma Nayak

Abstract

A series of benzothiazole linked phenylpyridopyrimidinones (8a-g) and their diones (9a-g) have been designed, synthesized and evaluated for their anticancer activity. Among the series one of the conjugate 8b showed significant cytotoxicity against human cervical cancer cell line ME-180 with IC50 value of 4.01μM. This compound was tested on the cell cycle perturbations and DNA damage. Flow cytometry analysis revealed that the compound 8b showed drastic cell cycle perturbations due to concentration dependent increase in the sub-G0 phase in ME-180 cell line. DNA fragmentation and Hoechst staining reveals that this compound induced cell death by apoptosis. Further caspase-3 and loss of mitochondrial membrane potential suggested that the compound induces cell death by apoptosis.

References

May 15, 2004·News in Physiological Sciences : an International Journal of Physiology Produced Jointly by the International Union of Physiological Sciences and the American Physiological Society·U Ziegler, P Groscurth

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Citations

Dec 3, 2014·European Journal of Medicinal Chemistry·Rangappa S KeriSrinivasa Budagumpi
Nov 25, 2014·Chemical Biology & Drug Design·Rajesh A RaneRajshekhar Karpoormath
Apr 13, 2017·Bioorganic & Medicinal Chemistry Letters·Thokhir B ShaikAhmed Kamal
Dec 4, 2019·Journal of Enzyme Inhibition and Medicinal Chemistry·Ali IrfanClaudiu T Supuran
Aug 29, 2021·Medicinal Research Reviews·Kritika LaxmikeshavNagula Shankaraiah

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Apoptosis

Apoptosis is a specific process that leads to programmed cell death through the activation of an evolutionary conserved intracellular pathway leading to pathognomic cellular changes distinct from cellular necrosis