Design, synthesis and biological evaluation of some novel quinazolinone derivatives as potent apoptotic inducers

Future Medicinal Chemistry
Raghad M NowarDalal A Abou El Ella

Abstract

Novel quinazolinone and triazinoquinazolinone derivatives were designed and synthesized as apoptotic inducers. Most of the synthesized compounds showed excellent antiproliferative activity against MCF-7 and HCT-116 cell lines, respectively. Compounds 7a, 8a, 8d, 14a and 14d were superior to doxorubicin as activators of caspases 3, 8 and 9 in HCT-116 cell line. The most potent caspase inducers, 8d and 14a showed cell cycle arrest mainly in G1 and S phase, respectively and increased the levels of p53, Bax and the Bax/Bcl-2 ratio compared with doxorubicin in HCT-116 cells with excellent selectivity against CCD-18Co human colon normal cell line. The synthesized compounds can be considered as potent apoptotic inducers interfering with extrinsic and intrinsic apoptotic pathways.

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Citations

Aug 20, 2019·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Rasha Mohamed HassanMohamed Nabil Aboul-Enein
May 9, 2021·Chemical Biology & Drug Design·Poonam YadavAnkur Vaidya

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