Haytham Tawfik

Scopus Publications

Isatin-triazole/imidazole hybrids as dual CDK2/VEGFR2 inhibitors with potent anti-cancer activity: design, synthesis, and biological evaluations
Zainab M. Elsayed, Marwa Balaha, Haytham O. Tawfik, Eman F. Khaleel, Moataz A. Shaldam, Ahmed T. Negmeldin, Ghada H. Al-Ansary, Diaaeldin M. Elimam, Yasser M. Omar, Viviana di Giacomo, Wagdy M. Eldehna
Bioorganic Chemistry, 2026
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, Haytham O. Tawfik, Moataz A. Shaldam
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, Anwar A. El‐Hamaky, Nourhan A. Khattab, Ahmed K. B. A. W. Farouk, Moataz A. Shaldam, Wagdy M. Eldehna, Mohamed S. Nafie
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.
Pyrazole–triazole hybrids as kinase-triad inhibitors: a triple-target strategy for synergistic anticancer therapy
Mahmoud S. Elkotamy, Mohamed K. Elgohary, Mariam M. Fakhry, Mohamed E. Albakri, Abdelrahman A. Naglah, Abdulrahman A. Almehizia, Ahmed M. Naglah, Mohamed Fares, Haytham O. Tawfik, Wagdy M. Eldehna, Hatem A. Abdel-Aziz
Rsc Medicinal Chemistry, 2026
The ongoing issue of drug resistance and the lack of specificity in existing cancer treatments highlight the necessity for innovative multi-target agents.
Thiazole-Semicarbazone Hybrids as Dual-Stage Inhibitors of Leishmania major Growth: Design, Synthesis, and Mechanistic Insights
Moataz A. Shaldam, Haytham O. Tawfik, Abdelrahman I. Zain‐Alabdeen, Rehan Monir, Mohamed R. Elnagar, Sherry N. Nasralla, Tamer M. Ibrahim, Wagdy M. Eldehna, Adnan A. Bekhit, Heba A. Elsebaie
Drug Development Research, 2026
As a neglected tropical disease, Leishmaniasis continues to pose a serious threat to world health, especially in areas with limited resources. There is a pressing need for safer and more effective antileishmanial drugs due to the limited efficacy, toxicity, and rising resistance of available agents. We report the rational design, synthesis, and biological evaluation of a novel series of 15 hybrid compounds ( 3a‐o ), utilizing the thiazole and semicarbazone pharmacophores, two privileged scaffolds recognized for their wide range of biological activity. Both intracellular amastigote and promastigote forms of Leishmania major were used to test the synthesized compounds' antileishmanial potential. With IC₅₀ values ranging from 2.97 to 10.18 µM against promastigotes and from 3.47 to 12.36 µM against amastigotes, a number of compounds demonstrated greater activity than the reference medication miltefosine. Selectivity indices revealed that compounds 3c , 3d , 3h , and 3i were the most potent, exhibiting a desirable balance between efficacy and cytotoxicity. The robust binding affinities and consistent interactions of these lead compounds inside the PTR1 and DHFR active sites were further supported by in silico docking. In conclusion, this study presents a novel chemotype that shows great promise for future advancement as a potent and focused antileishmanial treatment.
Exploring pyrazoline-thiophene hybrids as CDK2 inhibitors: synthesis, mechanism, biological studies, and computational insights
Heba M. Abosalim, Tarek F. El-Moselhy, Nabaweya Sharafeldin, Mohamed S. Nafie, Mohamed K. Diab, Mervat H. El-Hamamsy, Haytham O. Tawfik
Rsc Medicinal Chemistry, 2026
Novel pyrazoline-linked thiophenes were synthesized as anticancer agents. Lead compound 4p showed sub-micromolar cytotoxicity, induced CDK2-mediated apoptosis and cell-cycle arrest, and reduced tumor burden in vivo with low toxicity.
Synthesis of new trans-ferulic acid derivatives as potential anticancer agents and VEGFR-2 inhibitors
Asmaa N. Mohie, Mahmoud A. Doheim, Ragab A. El Masry, Ayman M. Gomaa, Rofaida Salem, Haytham O. Tawfik, Wagdy M. Eldehna
Rsc Medicinal Chemistry, 2026
By using –OH blocking, seven TFA derivatives were created. Compound 4e regulated AFP, BCL-2, caspase-3, and P53, inhibited VEGFR-2 in docking, and exhibited the maximum cytotoxicity against HepG2, Hep3B, and Huh7 with a safe profile.
Piperidine-based small molecules as dual-stage antileishmanial agents targeting parasite folate pathway
Tarfah Al-Warhi, Haytham O. Tawfik, Nermeen M. Rashad, Moataz A. Shaldam, Sherry N. Nasralla, Tamer M. Ibrahim, Adnan A. Bekhit, Wagdy M. Eldehna
Bioorganic Chemistry, 2026
Discovery of enaminone-linked benzofuran derivatives as dual VEGFR-2/hCA IX inhibitors exhibiting hypoxia-mediated chemosensitization
Wagdy M. Eldehna, Zainab M. Elsayed, Mohamed R. Elnagar, Andrea Ammara, Mahmoud S. Elkotamy, Rehan Monir, Alessio Nocentini, Mohammed M. Al-Sanea, Claudiu T. Supuran, Haytham O. Tawfik, Hatem A. Abdel-Aziz, Ahmed T. Negmeldin
Rsc Medicinal Chemistry, 2026
The overexpression of VEGFR-2 and carbonic anhydrase IX (hCA IX), two proven therapeutic targets in aggressive malignancies, is closely associated with hypoxia-driven tumor growth.
Harnessing benzofuran scaffolds: A journey through design, synthesis, and biological discovery toward safer anti-diabetic and anti-oxidant candidates
Mohamed K. Elgohary, Mahmoud S. Elkotamy, Mariam M. Fakhry, Mahmoud Abdelrahman Alkabbani, Abdelhameed Abubakr, Abdallah M. Hamdy, Abdel-Aziz S. Shatat, Rania S.M. Ismail, Aya Mohamed Ahmed Ibrahim, Abdulrahman A. Almehizia, Ahmed M. Naglah, Mayada H. Mohamed, Hazem A. Ghabbour, Haytham O. Tawfik, Wagdy M. Eldehna, Hatem A. Abdel-Aziz
European Journal of Medicinal Chemistry, 2026
Pharmacophore modeling: advances and pitfalls
Mahmoud Y. Elsaka, M. Modather Taha, Amr Tayel, Haytham O. Tawfik, Mahmoud A. A. Ibrahim, Tamer Shoeib
Frontiers in Molecular Biosciences, 2026
Potential of MAO-B Inhibitors with Multi-target Inhibition and Antioxidant Properties for the Treatment of Neurodegenerative Disorders
Moataz A. Shaldam, Simone Carradori, Francesco Melfi, Paolo Guglielmi, Francesca Diomede, Maurizio piattelli, Haytham O. Tawfik
Mini Reviews in Medicinal Chemistry, 2026
Patents involving monoamine oxidase (MAO): a comprehensive update (2022–2025) on its inhibitors and applications
Moataz A. Shaldam, Simone Carradori, Marwa Balaha, Paolo Guglielmi, Francesca Diomede, Ilaria D’Agostino, Haytham O. Tawfik
Expert Opinion on Therapeutic Patents, 2026
Development of novel chalcone-based quinazoline derivatives as dual VEGFR-2 and EGFR inhibitors
Zainab M. Elsayed, Haytham O. Tawfik, Loah R. Hemeda, Mohamed S. Nafie, Hadia Almahli, Rehan Monir, Ikhlas A. Sindi, Eslam B. Elkaeed, Mostafa M. Elbadawi, Mahmoud A. El Hassab, Wagdy M. Eldehna
Rsc Medicinal Chemistry, 2026
Discovery of potent bisindole-based pyrazolopyridine derivatives as topoisomerase inhibitors: DNA damage induction and synergistic antileukemic activity
Wagdy M. Eldehna, Haytham O. Tawfik, Denisa Veselá, Miroslav Peřina, Ahmed T. Negmeldin, Zainab M. Elsayed, Taghreed A. Majrashi, Veronika Vojáčková, Mostafa M. Elbadawi, Moataz A. Shaldam, Vladimír Kryštof, Hatem A. Abdel-Aziz
Frontiers in Pharmacology, 2026
Synthesis and Biological Evaluation of Imidazopyridine-Isatin Hybrids as Inhibitors of Leishmania major Growth
Mahmoud El Hassab, Wagdy Eldehna, Zainab Elsayed, Mostafa Elbadawi, Ahmed Negmeldin, Marwa Balaha, Sherry Nasralla, Rehan Monir, Tamer Ibrahim, Manabu Abe, Haytham Tawfik, Adnan Bekhit, Loah Hemeda
Drug Design Development and Therapy, 2026
Identification of Benzenesulfonamide-Containing Thiazolidine-2,4-Dione Derivatives as Novel Carbonic Anhydrase II and VII Inhibitors with Anti-Epileptic Activity
Mohamed M. Eldesouki, Mahmoud Abdelrahman Alkabbani, Mohammed S. Taghour, Andrea Ammara, Diaaeldin M. Elimam, Alaa Elwan, Rehan Monir, Kamyar Afarinkia, Alessio Nocentini, Claudiu T. Supuran, Haytham O. Tawfik, Wagdy M. Eldehna
Journal of Medicinal Chemistry, 2025
Next-Generation Proteolysis-Targeting Chimeras in Precision Oncology: Multifunctional Designs, Emerging Modalities, and Translational Prospects in Targeted Protein Degradation
Mohamed S. Nafie, Mohamed K. Diab, Asmaa S. A. Yassen, Amany M. Elshamy, Mohamed R. El Tohamy, Haytham O. Tawfik, Sherif Ashraf Fahmy
Drug Development Research, 2025
Discovery of Novel Piperidinyl-Based Benzoxazole Derivatives as Anticancer Agents Targeting VEGFR-2 and c-Met Kinases
Wagdy M. Eldehna, Zainab M. Elsayed, Mohamed R. Elnagar, Ahmed H. El-Said, Taghreed A. Majrashi, Ahmed T. Negmeldin, Abdulrahman M. Saleh, Ranza Elrayess, Khaled A. Elnahriry, Zhi-Long Chen, Mohamed Elagawany, Haytham O. Tawfik
Pharmaceuticals, 2025
Molecular hybrids integrated with Benzofuran, 1,2,3-Triazole and Pyrazole structural motifs: Design, synthesis, biological evaluation, and in vivo studies
Wagdy M. Eldehna, Mahmoud Abdelrahman Alkabbani, Mahmoud Rashed, Zainab M. Elsayed, Kawther Magdy Ibrahim, Taghreed A. Majrashi, Rofaida Salem, Haytham O. Tawfik
Bioorganic Chemistry, 2025
Click synthesis of some novel benzo[d]thiazole–1,2,3-triazole hybrid compounds with benzamide and/or benzoate tethers as EGFR-dependent signaling inhibitors against breast cancer
Mosa Alsehli, Mohamed S. Nafie, Nader R. Albujuq, Sanaa Bardaweel, Ateyatallah Aljuhani, Haytham O. Tawfik, Shaya Yahya Alraqa, Mohamed K. Diab, Nadjet Rezki, Mohamed Reda Aouad
Rsc Medicinal Chemistry, 2025
Identification of isatin-triazole-benzenesulfonamide hybrids as dual hCA IX/XII and c-met inhibitors with hypoxia-mediated chemo-sensitizing activity
Wagdy M. Eldehna, Mohamed R. Elnagar, Simone Giovannuzzi, Amr Tayel, Maha-Hamadien Abdulla, Noura S. Alhassan, Moataz A. Shaldam, Alessio Nocentini, Claudiu T. Supuran, Haytham O. Tawfik
Bioorganic Chemistry, 2025
Development of New Pyrazolo [3,4-b]Pyridine Derivatives as Potent Anti-Leukemic Agents and Topoisomerase IIα Inhibitors with Broad-Spectrum Cytotoxicity
Wagdy M. Eldehna, Haytham O. Tawfik, Denisa Veselá, Veronika Vojáčková, Ahmed T. Negmeldin, Zainab M. Elsayed, Taghreed A. Majrashi, Petra Krňávková, Mostafa M. Elbadawi, Moataz A. Shaldam, Ghada H. Al-Ansary, Vladimír Kryštof, Hatem A. Abdel-Aziz
Pharmaceuticals, 2025
Innovative design and synthesis of dual-acting hCA IX/CDK-2 inhibitors through hetero ring fused pyrimidine utilization for cutting-edge anticancer therapy: Zein nanoparticles for in vivo lung cancer treatment
Heba M. Abosalim, Tarek F. El-Moselhy, Nabaweya Sharafeldin, Simone Giovannuzzi, Paloma Begines, Mohamed S. Nafie, Sherif Ashraf Fahmy, Mohamed K. Diab, Asaad Babker, Claudiu T. Supuran, Mervat H. El-Hamamsy, Haytham O. Tawfik
Bioorganic Chemistry, 2025
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
Identification of Novel Triazole–Pyrazole Conjugates as Potential Anticonvulsant Agents: Synthesis and Biological Evaluations
Wagdy M. Eldehna, Mahmoud Abdelrahman Alkabbani, Zainab M. Elsayed, Kawther Magdy Ibrahim, Taghreed A Majrashi, Mohamed Elagawany, Rofaida Salem, Hatem A. Abdel-Aziz, Haytham O. Tawfik
ACS Chemical Neuroscience, 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, Eman F. Khaleel, Mohammad M. Al-Sanea, Mahmoud F. Abo-Ashour, Yosra S.R. Elnaggar, Alessio Nocentini, Claudiu T. Supuran, Haytham O. Tawfik
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, Eslam Roshdy, Mohammad M. Al-Sanea, Mostafa M. Elbadawi, Manabu Abe, Wagdy M. Eldehna, Hatem A. Abdel-Aziz, Haytham O. Tawfik
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, Mahmoud A. El Hassab, Zainab M. Elsayed, Yosra S.R. Elnaggar, Ahmed A. Al-Karmalawy, Viviana di Giacomo, Marwa Balaha
Bioorganic Chemistry, 2025
Targeted synthesis of a trimethoxyphenyltetrahydropyrimidine analogue designed as a DNA intercalator: in silico, multi-spectroscopic, thermodynamic, and in vitro approaches
Ahmed A. Al-Karmalawy, Ayman Abo Elmaaty, Galal Magdy, Aya Saad Radwan, Radwan Alnajjar, Moataz A. Shaldam, Arwa Omar Al Khatib, Salem Salman Almujri, Abdullah Yahya Abdullah Alzahrani, Haytham O. Tawfik
Rsc Advances, 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, Noura S. Alhassan, Thamer Bin Traiki, Mohammad M. Al-Sanea, Anwar A. El-Hamaky, Ahmed A. Al-Karmalawy, Ahmed M. El Kerdawy, Manabu Abe, Haytham O. Tawfik
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, Nourhan A. Khattab, Rehab Badi, Abdelhameed Abubakr, Abdallah M. Hamdy, Mohamed Fares, Haytham O. Tawfik, Claudiu T. Supuran, Wagdy M. Eldehna, Moataz A. Shaldam
Journal of Medicinal Chemistry, 2025
Design and synthesis of novel substituted s-triazines tethered benzenesulfonamides as potential antimicrobial candidates: Antibiofilm and bacterial protein permeability assessments
Ahmed A. Al‐Karmalawy, Haytham O. Tawfik, Gharieb S. El‐Sayyad, Ayman Abo Elmaaty, Sobhy S. Abdel‐Fatah, Akhtar Atiya, Abdullah Yahya Abdullah Alzahrani, Arwa Omar Al Khatib, Mervat H. El‐Hamamsy, Heba A. Elsebaie
Archiv Der Pharmazie, 2025
Donepezil-based rational design of N-substituted quinazolinthioacetamide candidates as potential acetylcholine esterase inhibitors for the treatment of Alzheimer's disease: in vitro and in vivo studies
Ahmed A. Al-Karmalawy, Ahmed F. Mohamed, Heba Nasr Shalaby, Ayman Abo Elmaaty, Riham A. El-Shiekh, Mohamed A. Zeidan, Radwan Alnajjar, Abdullah Yahya Abdullah Alzahrani, Mohammed H. AL Mughram, Moataz A. Shaldam, Haytham O. Tawfik
Rsc Medicinal Chemistry, 2025
Design, synthesis, and evaluation of novel benzofuran and pyrazole-based derivatives as dual AChE/BuChE inhibitors with antioxidant properties for Alzheimer's disease management
Mahmoud S. Elkotamy, Mohamed K. Elgohary, Mahmoud Abdelrahman Alkabbani, Mohamed M. Hefina, Haytham O. Tawfik, Mohamed Fares, Wagdy M. Eldehna, Hatem A. Abdel-Aziz
European Journal of Medicinal Chemistry, 2025
Coronaviruses papain-like proteases and their inhibitors
Ahmed E. Elsawi, Haytham O. Tawfik, Wagdy M. Eldehna
Enzymes, 2025
An overview of recent advancements in small molecules suppression of oncogenic signaling of K-RAS: an updated review
Ahmed Sabt, Haytham O. Tawfik, Eman F. Khaleel, Rehab Mustafa Badi, Hoda Atef Abdelsattar Ibrahim, Eslam B. Elkaeed, Wagdy M. Eldehna
Molecular Diversity, 2024
Muti-target rationale design of novel substituted N-phenyl-2-((6-phenylpyridazin-3-yl)thio)acetamide candidates as telomerase/JAK1/STAT3/TLR4 inhibitors: In vitro and in vivo investigations
Moataz A. Shaldam, Mai H.A. Mousa, Haytham O. Tawfik, Ahmed M. El-Dessouki, Marwa Sharaky, Mohamed M. Saleh, Abdullah Yahya Abdullah Alzahrani, Sana Ben Moussa, Ahmed A. Al-Karmalawy
Bioorganic Chemistry, 2024
Identification of indole-grafted pyrazolopyrimidine and pyrazolopyridine derivatives as new anti-cancer agents: Synthesis, biological assessments, and molecular modeling insights
Wagdy M. Eldehna, Haytham O. Tawfik, Maha-Hamadien Abdulla, Mohamed S. Nafie, Heba Aref, Moataz A. Shaldam, Noura S. Alhassan, Omar Al Obeed, Zainab M. Elsayed, Hatem A. Abdel-Aziz
Bioorganic Chemistry, 2024
Unveiling the potential of isatin-grafted phenyl-1,2,3-triazole derivatives as dual VEGFR-2/STAT-3 inhibitors: Design, synthesis and biological assessments
Heba A. Elsebaie, Maha-Hamadien Abdulla, Zainab M. Elsayed, Moataz A. Shaldam, Haytham O. Tawfik, Samar N. Morsy, Mansoor-Ali Vaali Mohammed, Thamer Bin Traiki, Eslam B. Elkaeed, Hatem A. Abdel-Aziz, Wagdy M. Eldehna
Bioorganic Chemistry, 2024
Fragment-based design and synthesis of coumarin-based thiazoles as dual c-MET/STAT-3 inhibitors for potential antitumor agents
Bassem H. Naguib, Heba A. Elsebaie, Mohamed S. Nafie, Samy Mohamady, Nader R. Albujuq, Aya Samir Ayed, Dina Nada, Ahmed F. Khalil, Salma M. Hefny, Haytham O. Tawfik, Moataz A. Shaldam
Bioorganic Chemistry, 2024
Novel sulfonamide-tethered Schiff bases as anti-proliferative agents with VEGFR-2 inhibitory activity: Synthesis, biological assessment, and molecular dynamic simulations
Moataz A. Shaldam, Maha-Hamadien Abdulla, Andrea Angeli, Salma M. Hefny, Eman M. El-labbad, Abdullah Bin Obeed, Noura S. Alhassan, Claudiu T. Supuran, Wagdy M. Eldehna, Haytham O. Tawfik
Journal of Molecular Structure, 2024
A new framework for novel analogues of pazopanib as potent and selective human carbonic anhydrase inhibitors: Design, repurposing rational, synthesis, crystallographic, in vivo and in vitro biological assessments
Salma M. Hefny, Tarek F. El-Moselhy, Nabaweya El-Din, Andrea Ammara, Andrea Angeli, Marta Ferraroni, Ahmed M. El-Dessouki, Moataz A. Shaldam, Galal Yahya, Ahmed A. Al-Karmalawy, Claudiu T. Supuran, Haytham O. Tawfik
European Journal of Medicinal Chemistry, 2024
Rationale design of novel substituted 1,3,5-triazine candidates as dual IDH1(R132H)/ IDH2(R140Q) inhibitors with high selectivity against acute myeloid leukemia: In vitro and in vivo preclinical investigations
Haytham O. Tawfik, Mai H.A. Mousa, Mohamed Y. Zaky, Ahmed M. El-Dessouki, Marwa Sharaky, Omeima Abdullah, Mervat H. El-Hamamsy, Ahmed A. Al-Karmalawy
Bioorganic Chemistry, 2024
Drosophila melanogaster as a model organism for diabetes II treatment by the ethyl acetate fraction of Atriplex halimus L.
Omnia Montaser, Mona El‐Aasr, Haytham O. Tawfik, Wesam S. Meshrif, Hanaa Elbrense
Journal of Experimental Zoology Part A Ecological and Integrative Physiology, 2024
Discovery of new 1,3-diphenylurea appended aryl pyridine derivatives as apoptosis inducers through c-MET and VEGFR-2 inhibition: design, synthesis, in vivo and in silico studies
Heba A. Elsebaie, Mohamed S. Nafie, Haytham O. Tawfik, Amany Belal, Mohammed M. Ghoneim, Ahmad J. Obaidullah, Salwa Shaaban, Abdelmoneim A. Ayed, Mohamed El-Naggar, Ahmed B. M. Mehany, Moataz A. Shaldam
Rsc Medicinal Chemistry, 2024
Discovery and Mechanistic Studies of Dual-Target Hits for Carbonic Anhydrase IX and VEGFR-2 as Potential Agents for Solid Tumors: X-ray, In Vitro, In Vivo, and In Silico Investigations of Coumarin-Based Thiazoles
Salma M. Hefny, Tarek F. El-Moselhy, Nabaweya El-Din, Simone Giovannuzzi, Thamer Bin Traiki, Mansoor-Ali Vaali-Mohammed, Ahmed M. El-Dessouki, Koki Yamaguchi, Masaharu Sugiura, Moataz A. Shaldam, Claudiu T. Supuran, Maha-Hamadien Abdulla, Wagdy M. Eldehna, Haytham O. Tawfik
Journal of Medicinal Chemistry, 2024
Tailored horseshoe-shaped nicotinonitrile scaffold as dual promising c-Met and Pim-1 inhibitors: Design, synthesis, SAR and in silico study
Samy Mohamady, Ahmed F. Khalil, Bassem H. Naguib, Mohamed S. Nafie, Haytham O. Tawfik, Moataz A. Shaldam
Bioorganic Chemistry, 2024
Development of new thieno[2,3-d]pyrimidines as dual EGFR and STAT3 inhibitors endowed with anticancer and pro-apoptotic activities
Heba A. Elsebaie, Tarek F. El-Moselhy, Eman A. El-Bastawissy, Kamel M. Elberembally, Rehab Mustafa Badi, Eslam B. Elkaeed, Moataz A. Shaldam, Wagdy M. Eldehna, Haytham O. Tawfik
Bioorganic Chemistry, 2024
Discovery of Novel Pyridazine-Tethered Sulfonamides as Carbonic Anhydrase II Inhibitors for the Management of Glaucoma
Haytham O. Tawfik, Mohamed M. Saleh, Andrea Ammara, Eman F. Khaleel, Rehab Badi, Yomna T. T. Khater, Rabab A. Rasheed, Ahmed A. Attia, Salma M. Hefny, Eslam B. Elkaeed, Alessio Nocentini, Claudiu T. Supuran, Wagdy M. Eldehna, Moataz A. Shaldam
Journal of Medicinal Chemistry, 2024
Lead Optimization of BIBR1591 To Improve Its Telomerase Inhibitory Activity: Design and Synthesis of Novel Four Chemical Series with In Silico, In Vitro, and In Vivo Preclinical Assessments
Ahmed A. Al-Karmalawy, Mai H. A. Mousa, Marwa Sharaky, Mai A. E. Mourad, Ahmed M. El-Dessouki, Amir O. Hamouda, Radwan Alnajjar, Abdelmoneim A. Ayed, Moataz A. Shaldam, Haytham O. Tawfik
Journal of Medicinal Chemistry, 2024
Identification of 3-(5-cyano-6-oxo-pyridin-2-yl)benzenesulfonamides as novel anticancer agents endowed with EGFR inhibitory activity
Moataz A. Shaldam, Ahmed F. Khalil, Hadia Almahli, Maiy Y. Jaballah, Andrea Angeli, Eman F. Khaleel, Rehab Mustafa Badi, Eslam B. Elkaeed, Claudiu T. Supuran, Wagdy M. Eldehna, Haytham O. Tawfik
Archiv Der Pharmazie, 2024
Evaluating the ability of some natural phenolic acids to target the main protease and AAK1 in SARS COV-2
Heba I. Ghamry, Amany Belal, Mohamed Kandeel El-Ashrey, Haytham O. Tawfik, Reem I. Alsantali, Ahmad J. Obaidullah, Ahmed A. El-Mansi, Doaa Abdelrahman
Scientific Reports, 2023
Novel fused imidazotriazines acting as promising top. II inhibitors and apoptotic inducers with greater selectivity against head and neck tumors: Design, synthesis, and biological assessments
Ahmed A. Al-Karmalawy, Mahmoud Rashed, Marwa Sharaky, Hamada S. Abulkhair, Mohamed M. Hammouda, Haytham O. Tawfik, Moataz A. Shaldam
European Journal of Medicinal Chemistry, 2023
Novel 4-(2-arylidenehydrazineyl)thienopyrimidine derivatives as anticancer EGFR inhibitors: Design, synthesis, biological evaluation, kinome selectivity and in silico insights
Heba A. Elsebaie, Eman A. El-Bastawissy, Kamel M. Elberembally, Eman F. Khaleel, Rehab Mustafa Badi, Moataz A. Shaldam, Wagdy M. Eldehna, Haytham O. Tawfik, Tarek F. El-Moselhy
Bioorganic Chemistry, 2023
2,4-Diaryl-pyrimido[1,2-a]benzimidazole derivatives as novel anticancer agents endowed with potent anti-leukemia activity: Synthesis, biological evaluation and kinase profiling
Moataz A. Shaldam, Denisa Hendrychová, Radwan El-Haggar, Veronika Vojáčková, Taghreed A. Majrashi, Eslam B. Elkaeed, Nicolas Masurier, Vladimír Kryštof, Haytham O. Tawfik, Wagdy M. Eldehna
European Journal of Medicinal Chemistry, 2023
Terminators or Guardians? Design, Synthesis, and Cytotoxicity Profiling of Chalcone-Sulfonamide Hybrids
Shaimaa M. Aboukhatwa, Peter A. Sidhom, Andrea Angeli, Claudiu T. Supuran, Haytham O. Tawfik
ACS Omega, 2023
Papaverinol-N-Oxide: A Microbial Biotransformation Product of Papaverine with Potential Antidiabetic and Antiobesity Activity Unveiled with In Silico Screening
Duaa Eliwa, Amal Kabbash, Mona El-Aasr, Haytham O. Tawfik, Gaber El-Saber Batiha, Mohamed H. Mahmoud, Michel De Waard, Wagdy M. Eldehna, Abdel-Rahim S. Ibrahim
Molecules, 2023
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, Anwar A. El-Hamaky, Mohamed A. Saleh, Ahmed Elkamhawy, Haytham O. Tawfik
Journal of Medicinal Chemistry, 2023
Evaluation of Zamia floridana A. DC. Leaves and Its Isolated Secondary Metabolites as Natural Anti-Toxoplasma and Anti-Cancer Agents Using In Vitro and In Silico Studies
Hosam M. El-Seadawy, Kamilia A. Abo El-Seoud, Mona El-Aasr, Haytham O. Tawfik, Wagdy M. Eldehna, Amany E. Ragab
Metabolites, 2023
Synthesis, crystallographic, DNA binding, and molecular docking/dynamic studies of a privileged chalcone-sulfonamide hybrid scaffold as a promising anticancer agent
Moataz Shaldam, Haytham Tawfik, Heba Elmansi, Fathalla Belal, Koki Yamaguchi, Masaharu Sugiura, Galal Magdy
Journal of Biomolecular Structure and Dynamics, 2023
Recruitment of hexahydroquinoline as anticancer scaffold targeting inhibition of wild and mutants EGFR (EGFRWT, EGFRT790M, and EGFRL858R)
Mahmoud G. Abo Al-Hamd, Haytham O. Tawfik, Omeima Abdullah, Koki Yamaguchi, Masaharu Sugiura, Ahmed B. M. Mehany, Mervat H. El-Hamamsy, Tarek F. El-Moselhy
Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
LC-MS/MS metabolomics profiling of Glechoma hederacea L. methanolic extract; in vitro antimicrobial and in vivo with in silico wound healing studies on Staphylococcus aureus infected rat skin wound
Mona El-Aasr, Toshihiro Nohara, Tsuyushi Ikeda, Sally E. Abu-Risha, Engy Elekhnawy, Haytham O. Tawfik, Nagwa Shoeib, Ghada Attia
Natural Product Research, 2023
Investigating the potential anticancer activities of antibiotics as topoisomerase II inhibitors and DNA intercalators: in vitro, molecular docking, molecular dynamics, and SAR studies
Faten Farouk, Ayman Abo Elmaaty, Ahmed Elkamhawy, Haytham O. Tawfik, Radwan Alnajjar, Mohammed A. S. Abourehab, Mohamed A. Saleh, Wagdy M. Eldehna, Ahmed A. Al‐Karmalawy
Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Discovery of sulfonamide-tethered isatin derivatives as novel anticancer agents and VEGFR-2 inhibitors
Moataz A. Shaldam, Hadia Almahli, Andrea Angeli, Rehab Mustafa Badi, Eman F. Khaleel, Abdelrahman I. Zain-Alabdeen, Zainab M. Elsayed, Eslam B. Elkaeed, Rofaida Salem, Claudiu T. Supuran, Wagdy M. Eldehna, Haytham O. Tawfik
Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Nicotinonitrile-derived apoptotic inducers: Design, synthesis, X-ray crystal structure and Pim kinase inhibition
Shaimaa M. Aboukhatwa, Amera O. Ibrahim, Hiroshi Aoyama, Ahmed S. Al-Behery, Moataz A. Shaldam, Ghada El-Ashmawy, Haytham O. Tawfik
Bioorganic Chemistry, 2022
Toxoplasmocidal and Cytotoxic Activities Guided Isolation and Characterization of an Undescribed Bioflavonoid-di-C-glucoside from Cycas rumphii Miq. Cultivated in Egypt
Hosam M. El-Seadawy, Kamilia A. Abo El-Seoud, Mona El-Aasr, Haytham O. Tawfik, Amany E. Ragab
Plants, 2022
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, Yulia A. Gladilina, Dmitry D. Zhdanov, Mervat H. El-Hamamsy
Pharmaceuticals, 2022
Discovery of new carbonic anhydrase IX inhibitors as anticancer agents by toning the hydrophobic and hydrophilic rims of the active site to encounter the dual-tail approach
Haytham O. Tawfik, Andrea Petreni, Claudiu T. Supuran, Mervat H. El-Hamamsy
European Journal of Medicinal Chemistry, 2022
Dependence on linkers’ flexibility designed for benzenesulfonamides targeting discovery of novel hCA IX inhibitors as potent anticancer agents
Haytham O. Tawfik, Amany Belal, Mohammed A. S. Abourehab, Andrea Angeli, Alessandro Bonardi, Claudiu T. Supuran, Mervat H. El-Hamamsy
Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Novel 3-(6-methylpyridin-2-yl)coumarin-based chalcones as selective inhibitors of cancer-related carbonic anhydrases IX and XII endowed with anti-proliferative activity
Haytham O. Tawfik, Moataz A. Shaldam, Alessio Nocentini, Rofaida Salem, Hadia Almahli, Sara T. Al-Rashood, Claudiu T. Supuran, Wagdy M. Eldehna
Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Discovery of new symmetrical and asymmetrical nitrile-containing 1,4-dihydropyridine derivatives as dual kinases and P-glycoprotein inhibitors: synthesis, in vitro assays, and in silico studies
Mohamed H. Saad, Tarek F. El-Moselhy, Nabaweya S, El-Din, Ahmed B. M. Mehany, Amany Belal, Mohammed A. S. Abourehab, Haytham O. Tawfik, Mervat H. El-Hamamsy
Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
The plausible mechanisms of tramadol for treatment of COVID-19
Nahla E. El-Ashmawy, Abdel-Halim A. Lashin, Kamal M. Okasha, Amal M. Abo Kamer, Tarek M. Mostafa, Mona El-Aasr, Ahmed E. Goda, Yusuf A. Haggag, Haytham O. Tawfik, Mariam A. Abo-Saif
Medical Hypotheses, 2021
Corrigendum to “Design, synthesis, and bioactivity of dihydropyrimidine derivatives as kinesin spindle protein inhibitors” [Bioorg. Med. Chem. 27 (2019) 115126] (Bioorganic & Medicinal Chemistry (2019) 27(23), (S0968089619311599), (10.1016/j.bmc.2019.115126))
Haytham O. Tawfik, Tarek F. El-Moselhy, Nabaweya S. El-Din, Mervat H. El-Hamamsy
Bioorganic and Medicinal Chemistry, 2020
Design, synthesis, and molecular docking study of new monastrol analogues as kinesin spindle protein inhibitors
Mervat H. El‐Hamamsy, Nabaweya A. Sharafeldin, Tarek F. El‐Moselhy, Haytham O. Tawfik
Archiv Der Pharmazie, 2020
Corrigendum to “Design, synthesis, and bioactivity of dihydropyrimidine derivatives as kinesin spindle protein inhibitors” [Bioorg. Med. Chem. 27 (2019) 115126](S0968089619311599)(10.1016/j.bmc.2019.115126)
Haytham O. Tawfik, Tarek F. El-Moselhy, Nabaweya S. El-Din, Mervat H. El-Hamamsy
Bioorganic and Medicinal Chemistry, 2020
Design, synthesis, and bioactivity of dihydropyrimidine derivatives as kinesin spindle protein inhibitors
Haytham O. Tawfik, Tarek F. El-Moselhy, Nabaweya S. El-Din, Mervat H. El-Hamamsy
Bioorganic and Medicinal Chemistry, 2019

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