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Anticancer Agents Med Chem. 2019 Sep 6. doi: 10.2174/1871520619666190906162537. [Epub ahead of print]

Synthesis of Substituted Cinnamido Linked Quinazolinone Congeners as Potential Anticancer Agents via Mitochondrial Dependent Intrinsic Apoptotic Pathway.

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Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad-500037. India.
Department of Regulatory Toxicology, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad-500037. India.
Fluoro-Agrochemicals, CSIR-Indian Institute of Chemical Technology, Hyderabad-500007. India.



The synthesis of novel heterocyclic scaffolds with amide functionality is a key research area due to their plethora of medicinal applications. Present study aims to explore the synthesis of new cinnamido linked quinazolinone congeners and their potential as anticancer agents.


Cytotoxicity evaluation, Cell cycle analysis, JC-1 staining, ROS, Annexin V assays, AO/EB, DAPI nuclear staining, Colony forming assay and Western blot analysis.


Among the synthesized compounds 5eb and 5fc have shown promising cytotoxic activity with an IC50 value of 3.89±1.01µM and 4.05±0.62µM against HeLa cell lines. Flow-cytometry analysis demonstrated that the compound 5eb arrest the sub-G1 phase of cell cycle and induce apoptosis. Furthermore the compound 5eb trigger the collapse of mitochondrial membrane potential (ΔѰm), which was assessed by JC-1 staining and also induce the generation of Reactive Oxygen Species. Increase in the expression of pro-apoptotic proteins such as Bax, p53, cleaved PARP and cleaved caspase-3 by 5eb confirms the activation of mitochondrial dependent intrinsic apoptosis pathway.


Our results suggest that compound 5eb and 5fc of cinnamido linked quinazolinone derivatives could serve as potential leads in the development of novel chemotherapeutic agents.


Quinazolinones; apoptosis mechanism; cinnamic acids; cinnamides; cytotoxicity

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