Anwar Amin El-Hamaky

Verified @pharm.tanta.edu.eg

Teaching assistant of Pharmaceutical Chemistry at Faculty of Pharmacy, University of Tanta

Anwar Amin El-Hamaky


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https://researchid.co/anwaramin

RESEARCH, TEACHING, or OTHER INTERESTS

Drug Discovery, Chemistry
10

Scopus Publications

180

Scholar Citations

8

Scholar h-index

8

Scholar i10-index

Scopus Publications

  • Biphenyl urea derivatives as novel GPX4 inhibitors: ferroptosis-mediated antiproliferative activity against CNS cancer cells
    Wagdy M. Eldehna, Salma M. Hefny, Heba A. Elsebaie, Heba Aref, Anwar A. El-Hamaky, et al.
    Bioorganic Chemistry, 2026
  • Molecular Boomerangs Against Cancer: Design, Synthesis, Biological Evaluation, and In Silico Study of Novel Dual PARP-1/EGFR Inhibitors
    Haytham O. Tawfik, Amr Tayel, Salma M. Hefny, Tarfah Al‐Warhi, Nada K. Sedky, et al.
    Drug Development Research, 2026
    A possible method for improving anti‐cancer efficacy is the combination of the inhibition of epidermal growth factor receptor (EGFR) and poly (ADP‐ribose) polymerase‐1 (PARP‐1). This work describes the rational design, synthesis, and complete characterization of a novel class of boomerang‐shaped dual PARP‐1/EGFR inhibitors ( 3a – o ). HepG‐2 and MDA‐MB‐231 cancer cell lines were used to test the synthesized compounds’ antiproliferative potential; MDA‐MB‐231 cells showed greater sensitivity. Compounds 3h , 3i , and 3j had the strongest cytotoxic effects among the series, with IC 50 values of 0.23, 0.90, and 1.40 µM, respectively, against MDA‐MB‐231 cells. Compared with the reference medications erlotinib and olaparib, compound 3h showed the highest dual inhibition (EGFR IC 50 = 1.62 µM and PARP‐1 IC 50 = 0.36 µM) in enzymatic experiments, demonstrating that these compounds effectively inhibited both EGFR and PARP‐1. Compound 3h strongly promoted apoptosis in MDA‐MB‐231 cells, increasing the total apoptotic population to 20.04% and causing G1‐phase cell‐cycle arrest, as determined by mechanistic studies. In vivo tumor growth inhibition trials showed a tumor inhibition rate (TIR%) of 41.4% for compound 3h compared to 48.8% for doxorubicin (DOX). Liver function biomarkers and hematological parameters remained within the acceptable levels following compound 3h treatment. The dual‐target activity of compound 3h was further validated by molecular docking and molecular dynamics simulations, which demonstrated persistent binding contacts within the active sites of PARP‐1 and EGFR.
  • Therapeutic targeting of ubiquitin-specific protease 7 (USP7): Mechanistic insights, dysregulation, and advances in drug discovery
    Anwar A. El-Hamaky, Mervat H. El-Hamamsy, Tarek F. El-Moselhy, Nabaweya Sharafeldin, Haytham O. Tawfik
    European Journal of Medicinal Chemistry, 2025
  • Development of isatin-functionalized benzenesulfonamides as novel carbonic anhydrase II and VII inhibitors with antiepileptic potential
    Wagdy M. Eldehna, Anwar A. El-Hamaky, Simone Giovannuzzi, Zainab M. Elsayed, Mahmoud Abdelrahman Alkabbani, et al.
    European Journal of Medicinal Chemistry, 2025
  • Triazole-functionalized benzofuran and benzothiophene semicarbazides as novel VEGFR-2-targeted anti-cancer agents
    Mohamed S. Nafie, Mariam I. Youssef, Anwar A. El-Hamaky, Zainab M. Elsayed, Eman F. Khaleel, et al.
    Bioorganic Chemistry, 2025
  • Novel benzofuran-conjugated indolin-2-ones as anticancer agents; design, synthesis, biological assessments, and molecular modeling insights
    Wagdy M. Eldehna, Haytham O. Tawfik, Mohamed S. Nafie, Omkulthom Al Kamaly, Anwar A. El-Hamaky, et al.
    Bioorganic Chemistry, 2025
  • Discovery of 1-phenyl-1,2,3-triazole ureas as dual VEGFR-2/JNK-1 type II kinase inhibitors targeting pancreatic cancer
    Wagdy M. Eldehna, Eslam Roshdy, Maha-Hamadien Abdulla, Abdelrahman I. Zain-Alabdeen, Moataz A. Shaldam, et al.
    International Journal of Biological Macromolecules, 2025
  • Shooting an Arrow against Convulsion: Novel Triazole-Grafted Benzenesulfonamide Derivatives as Carbonic Anhydrase II and VII Inhibitors
    Mohamed A. Zeidan, Mahmoud Abdelrahman Alkabbani, Simone Giovannuzzi, Eman F. Khaleel, Anwar A. El-Hamaky, et al.
    Journal of Medicinal Chemistry, 2025
    This study investigates new anticonvulsant substances that target the epilepsy-associated carbonic anhydrase isoforms II and VII. The 1,2,3-triazole with a benzenesulfonamide motif is present in the produced molecules. Of these, 5b and 5c exhibited remarkable selectivity and inhibitory efficacy toward hCA VII and hCA II over hCA I. The KI values of 5b and 5c were 6.3 and 10.1 nM, respectively, and 21.6 and 18.9 nM, respectively. In a pilocarpine-induced paradigm, in vivo assessments showed decreased seizure severity and susceptibility with delayed seizure onset and diminished intensity. The quick absorption and in vivo stability of 5b were demonstrated by pharmacokinetic investigations. Evaluations of toxicity showed no neurotoxic effects and a high safety margin (LD50 > 2000 mg/kg). Mechanistic research has shown effectiveness in maintaining neuronal integrity, reducing mTOR activation, and raising hippocampus KCC2 levels. Compound 5b's binding interactions with hCA II and hCA VII were clarified by docking and dynamics experiments.
  • Ligand-Based Design on the Dog-Bone-Shaped BIBR1532 Pharmacophoric Features and Synthesis of Novel Analogues as Promising Telomerase Inhibitors with in Vitro and in Vivo Evaluations
    Ahmed A. Al-Karmalawy, Mohamed S. Nafie, Moataz A. Shaldam, Ayman Abo Elmaaty, Samar A. Antar, et al.
    Journal of Medicinal Chemistry, 2023
    Telomerase is an outstanding biological target for cancer treatment. BIBR1532 is a non-nucleoside selective telomerase inhibitor; however, it experiences ineligible pharmacokinetics. Herein, we aimed to design new BIBR1532-based analogues as promising telomerase inhibitors. Therefore, two novel series of pyridazine-linked to cyclopenta[b]thiophene (8a-f) and tetrahydro-1-benzothiophene (9a-f) were synthesized. A quantitative real-time polymerase chain reaction was utilized to investigate the telomerase inhibitory activity of candidates. Notably, 8e and 9e exhibited the best inhibition profiles. Moreover, 8e showed strong antitumor effects against both MCF-7 and A549 cancer cell lines. The effects of 8e on the cell cycle and apoptosis were measured. Besides, 8e was evaluated for its in vivo antitumor activity using solid Ehrlich carcinoma. The reduction in both the tumor weight and volume was greater than doxorubicin. Also, molecular docking and ADME studies were performed. Finally, a SAR study was conducted to gain further insights into the different telomerase inhibition potentials upon variable structural modifications.
  • New Genetic Bomb Trigger: Design, Synthesis, Molecular Dynamics Simulation, and Biological Evaluation of Novel BIBR1532-Related Analogs Targeting Telomerase against Non-Small Cell Lung Cancer
    Haytham O. Tawfik, Anwar A. El-Hamaky, Eman A. El-Bastawissy, Kirill A. Shcherbakov, Alexander V. Veselovsky, et al.
    Pharmaceuticals, 2022
    Telomeres serve a critical function in cell replication and proliferation at every stage of the cell cycle. Telomerase is a ribonucleoprotein, responsible for maintaining the telomere length and chromosomal integrity of frequently dividing cells. Although it is silenced in most human somatic cells, telomere restoration occurs in cancer cells because of telomerase activation or alternative telomere lengthening. The telomerase enzyme is a universal anticancer target that is expressed in 85–95% of cancers. BIBR1532 is a selective non-nucleoside potent telomerase inhibitor that acts by direct noncompetitive inhibition. Relying on its structural features, three different series were designed, and 30 novel compounds were synthesized and biologically evaluated as telomerase inhibitors using a telomeric repeat amplification protocol (TRAP) assay. Target compounds 29a, 36b, and 39b reported the greatest inhibitory effect on telomerase enzyme with IC50 values of 1.7, 0.3, and 2.0 μM, respectively, while BIBR1532 displayed IC50 = 0.2 μM. Compounds 29a, 36b, and 39b were subsequently tested using a living-cell TRAP assay and were able to penetrate the cell membrane and inhibit telomerase inside living cancer cells. Compound 36b was tested for cytotoxicity against 60 cancer cell lines using the NCI (USA) procedure, and the % growth was minimally impacted, indicating telomerase enzyme selectivity. To investigate the interaction of compound 36b with the telomerase allosteric binding site, molecular docking and molecular dynamics simulations were used.

RECENT SCHOLAR PUBLICATIONS

  • Biphenyl urea derivatives as novel GPX4 inhibitors: ferroptosis-mediated antiproliferative activity against CNS cancer cells
    WM Eldehna, SM Hefny, HA Elsebaie, H Aref, AA El-Hamaky, HO Tawfik, ...
    Bioorganic Chemistry, 109714 , 2026
    2026
  • Therapeutic targeting of ubiquitin-specific protease 7 (USP7): mechanistic insights, dysregulation, and advances in drug discovery
    AA El-Hamaky, MH El-Hamamsy, TF El-Moselhy, N Sharafeldin, ...
    European Journal of Medicinal Chemistry 296, 117872 , 2025
    2025
    Citations: 11
  • Development of isatin-functionalized benzenesulfonamides as novel carbonic anhydrase II and VII inhibitors with antiepileptic potential
    WM Eldehna, AA El-Hamaky, S Giovannuzzi, ZM Elsayed, MA Alkabbani, ...
    European Journal of Medicinal Chemistry 292, 117706 , 2025
    2025
    Citations: 14
  • Triazole-functionalized benzofuran and benzothiophene semicarbazides as novel VEGFR-2-targeted anti-cancer agents
    MS Nafie, MI Youssef, AA El-Hamaky, ZM Elsayed, EF Khaleel, E Roshdy, ...
    Bioorganic Chemistry 163, 108702 , 2025
    2025
    Citations: 13
  • Novel benzofuran-conjugated indolin-2-ones as anticancer agents; design, synthesis, biological assessments, and molecular modeling insights
    WM Eldehna, HO Tawfik, MS Nafie, O Al Kamaly, AA El-Hamaky, ...
    Bioorganic Chemistry 160, 108494 , 2025
    2025
    Citations: 12
  • Discovery of 1-phenyl-1, 2, 3-triazole ureas as dual VEGFR-2/JNK-1 type II kinase inhibitors targeting pancreatic cancer
    WM Eldehna, E Roshdy, MH Abdulla, AI Zain-Alabdeen, MA Shaldam, ...
    International Journal of Biological Macromolecules 308, 142372 , 2025
    2025
    Citations: 11
  • Shooting an arrow against convulsion: novel Triazole-grafted Benzenesulfonamide derivatives as carbonic anhydrase II and VII inhibitors
    MA Zeidan, MA Alkabbani, S Giovannuzzi, EF Khaleel, AA El-Hamaky, ...
    Journal of Medicinal Chemistry 68 (8), 8873-8893 , 2025
    2025
    Citations: 17
  • Ligand-based design on the dog-bone-shaped BIBR1532 pharmacophoric features and synthesis of novel analogues as promising telomerase inhibitors with in vitro and in vivo …
    AA Al-Karmalawy, MS Nafie, MA Shaldam, AA Elmaaty, SA Antar, ...
    Journal of Medicinal Chemistry 66 (1), 777-792 , 2022
    2022
    Citations: 68
  • New Genetic Bomb Trigger: Design, Synthesis, Molecular Dynamics Simulation, and Biological Evaluation of Novel BIBR1532-Related Analogs Targeting Telomerase against Non-Small …
    MHEH Haytham O. Tawfik, Anwar A. El-Hamaky, Eman A. El-Bastawissy, Kirill A ...
    Pharmaceuticals 15 (4), 1-28 , 2022
    2022
    Citations: 34

MOST CITED SCHOLAR PUBLICATIONS

  • Ligand-based design on the dog-bone-shaped BIBR1532 pharmacophoric features and synthesis of novel analogues as promising telomerase inhibitors with in vitro and in vivo …
    AA Al-Karmalawy, MS Nafie, MA Shaldam, AA Elmaaty, SA Antar, ...
    Journal of Medicinal Chemistry 66 (1), 777-792 , 2022
    2022
    Citations: 68
  • New Genetic Bomb Trigger: Design, Synthesis, Molecular Dynamics Simulation, and Biological Evaluation of Novel BIBR1532-Related Analogs Targeting Telomerase against Non-Small …
    MHEH Haytham O. Tawfik, Anwar A. El-Hamaky, Eman A. El-Bastawissy, Kirill A ...
    Pharmaceuticals 15 (4), 1-28 , 2022
    2022
    Citations: 34
  • Shooting an arrow against convulsion: novel Triazole-grafted Benzenesulfonamide derivatives as carbonic anhydrase II and VII inhibitors
    MA Zeidan, MA Alkabbani, S Giovannuzzi, EF Khaleel, AA El-Hamaky, ...
    Journal of Medicinal Chemistry 68 (8), 8873-8893 , 2025
    2025
    Citations: 17
  • Development of isatin-functionalized benzenesulfonamides as novel carbonic anhydrase II and VII inhibitors with antiepileptic potential
    WM Eldehna, AA El-Hamaky, S Giovannuzzi, ZM Elsayed, MA Alkabbani, ...
    European Journal of Medicinal Chemistry 292, 117706 , 2025
    2025
    Citations: 14
  • Triazole-functionalized benzofuran and benzothiophene semicarbazides as novel VEGFR-2-targeted anti-cancer agents
    MS Nafie, MI Youssef, AA El-Hamaky, ZM Elsayed, EF Khaleel, E Roshdy, ...
    Bioorganic Chemistry 163, 108702 , 2025
    2025
    Citations: 13
  • Novel benzofuran-conjugated indolin-2-ones as anticancer agents; design, synthesis, biological assessments, and molecular modeling insights
    WM Eldehna, HO Tawfik, MS Nafie, O Al Kamaly, AA El-Hamaky, ...
    Bioorganic Chemistry 160, 108494 , 2025
    2025
    Citations: 12
  • Therapeutic targeting of ubiquitin-specific protease 7 (USP7): mechanistic insights, dysregulation, and advances in drug discovery
    AA El-Hamaky, MH El-Hamamsy, TF El-Moselhy, N Sharafeldin, ...
    European Journal of Medicinal Chemistry 296, 117872 , 2025
    2025
    Citations: 11
  • Discovery of 1-phenyl-1, 2, 3-triazole ureas as dual VEGFR-2/JNK-1 type II kinase inhibitors targeting pancreatic cancer
    WM Eldehna, E Roshdy, MH Abdulla, AI Zain-Alabdeen, MA Shaldam, ...
    International Journal of Biological Macromolecules 308, 142372 , 2025
    2025
    Citations: 11
  • Biphenyl urea derivatives as novel GPX4 inhibitors: ferroptosis-mediated antiproliferative activity against CNS cancer cells
    WM Eldehna, SM Hefny, HA Elsebaie, H Aref, AA El-Hamaky, HO Tawfik, ...
    Bioorganic Chemistry, 109714 , 2026
    2026