Staff Profile

Education

• • Bachelor
  • 2017
• • Master
  • 2020
  • Part I: VEGFR-2 inhibitors have been becoming one of the most therapeutic strategy for treatment of cancer diseases because of their critical role in preventing cancer growth and metastasis. Herein, new series of novel N-(1,3,4-thiadiazol-2-yl)furan-2-carboxamide derivatives were designed and synthesized based on the same essential pharmacophoric features of the reported VEGFR-2 inhibitors by adopting a hybridization of bioisosteric strategy. Antiproliferative activities were biologically evaluated against three human cancer cell lines (MCF-7, HCT-116 and PC-3) using MTT assay technique and doxorubicin was used as a positive control. Compounds, 6, 7, 11 and 14 were found to be significantly more potent than doxorubicin against all tested cell lines. Moreover, compounds, 6 and 11 proved to be the most active compounds with IC50 values of 6.58, 4.19, and 7.76 µM, and 6.41, 5.01, and 8.47 µM, respectively. The most active cytotoxic agents were further evaluated in vitro for their VEGFR-2 inhibitory activities. Among them, compounds, 11, 7 and 15 exhibited excellent inhibition against VEGFR-2 with IC50 values of 7.6±0.4, 9.4±0.8 and 8.2±0.4 µM, respectively, compared with pazopanib as control drug with IC50 value of 9.7±0.4 µM. Furthermore, structure-activity relationship (SAR) studies indicated the active methylene linker substituted with heteroaromatic ring enhances the antiproliferative activity. Besides, molecular docking studies were also performed and attributed the promising activity of this series to their hydrogen bonding interactions with the key amino acid residues, Glu885, Cys919 and Asp1026 and hydrophobic interactions with the VEGFR-2 binding site.   Part II: A series of new 1,2,4-triazole-3-thiones were synthesized by calm, benign, no risk, eco-friendly, and energy efficient sequential reaction methodology like grinding and ultrasonic (US). In addition, 1,2,4-triazoles were prepared under conventional method and comparative study was done. The synthesized 1,2,4-triazoles were complexed with Ni(II) to produce nanoparticles complexes (NPC's) with average particle size vary from 55 to 100 nm (using scanning electron microscope technique) with good yields via both US and conventional techniques. X-ray diffraction technique and spectra analysis techniques were used to confirm the square planer geometry of the synthesized NPC's. Antimicrobial activity of the prepared 1,2,4-triazoles and their nickel complexes were studied which evaluated a high activity with complexes instead their triazoles. Keywords: Isothiocyanate, Anticancer, VEGFR-2 inhibitors, 1,3,4-thiadiazole derivatives, Molecular docking, 1,2,4-triazole derivatives, green chemistry Nanoparticles, Organometallic, XRD.
• • Phd
  • 2023
  • Synthesis, and Pharmacological Evaluation of Some Novel Heterocyclic Compounds Derived from Aroyl isothiocyanates as Anticancer Agents

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