The research entitled. “Synthesis, docking study, and antitumor evaluation of benzamides and oxadiazole derivatives of 3-phenoxybenzoic acid as VEGFR-2 inhibitors” has been published by Dr. (Mohammed Hamza Haraz),

lecturer at the Faculty of Pharmacy
in “Drug development research” Journal which is classified in the (second) quarter of Scopus and Clarivate container.

The research included the current numerous limitations of chemotherapeutic agents, including lack of selectivity, development of unwanted side effects, and chemo-resistance. As a result, there is an unsatisfied need to develop new small molecules with minimal side effects and the ability to specifically target cancer cells”.
A new series of 3-phenoxybenzoic acid derivatives, including 1,3,4-oxadiazole derivatives (4a-d) and benzamide derivatives (5a-e) were synthesized; their chemical structures were confirmed by infrared spectroscopy, nuclear magnetic analysis (1HNMR and 13CNMR), and mass spectra; as well as their various physical and chemical properties were determined..
The biological efficacy of the synthesized compounds like antiproliferative activities were evaluated by assay. (MTT) Three compounds (4b, 4c, and 4d) showed cytotoxicity against two of the three cell lines tested, and five compounds (3, 4a, 5a, 5b, and 5e) were toxic to one cell line, while two compounds (5c and 5d) were not toxic to any of the three cell lines tested in the current study..
Based on the results of the binding score, MTT assay, and vascular endothelial growth factor receptor 2 (VEGFR-2) kinase activity data, compound 4d was selected for further biological investigation
Flow cytometry was used to determine the mode of cell death (apoptosis versus necrosis) and the effect on cell cycle progression. Compound 4d inhibited HepG2 hepatocellular carcinoma (HCC) in the G2/M phase and activated intrinsic and extrinsic apoptosis. In conclusion, compound 4d showed promising future potential as a potent inhibitor of VEGFR-2 tyrosine kinase..

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