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Discovery of new VEGFR-2 inhibitors based on bis([1, 2, 4]triazolo)[4,3-<i>a</i>:3',4'-<i>c</i>]quinoxaline derivatives as anticancer agents and apoptosis inducers

Nawaf A. Alsaif, Mohammed S. Taghour, Mohammed M. Alanazi, Ahmad J. Obaidullah, Abdulrahman A. Almehizia, Manal M. Alanazi, Saleh Aldawas, Alaa Elwan, Hazem Elkady

2021Journal of Enzyme Inhibition and Medicinal Chemistry63 citationsDOIOpen Access PDF

Abstract

arrested the HepG2 cell growth at the G2/M phase and induced apoptosis by 40.12% compared to the control cells (7.07%). As well, such compound showed a significant increase in the level of caspase-3 (1.36-fold), caspase-9 (2.80-fold), and BAX (1.65-fold), and exhibited a significant decrease in Bcl-2 level (2.63-fold).

Topics & Concepts

QuinoxalineChemistryApoptosisIC50StereochemistryLead compoundSorafenibIn vitroDocking (animal)Cytotoxic T cellCell cultureBiochemistryBiologyCancer researchOrganic chemistryMedicineNursingGeneticsHepatocellular carcinomaSynthesis and Biological EvaluationBioactive Compounds and Antitumor AgentsSynthesis and biological activity
Discovery of new VEGFR-2 inhibitors based on bis([1, 2, 4]triazolo)[4,3-<i>a</i>:3',4'-<i>c</i>]quinoxaline derivatives as anticancer agents and apoptosis inducers | Litcius