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Fathi Halaweish Research

Research Summary

My group conducts research on the structural, synthetic and medicinal chemistry of natural products. This includes molecular modeling, chemical and biological investigation and methods development for drug discovery of exceedingly small amounts of rare natural products using NMR, and mass spectrometry (MS), and synthesis of drug-like analogs for therapeutic areas using in silicon approaches.

We have developed several drug candidates and expertise in Hit-to-Lead optimization (computational support and/or synthetic medicinal chemistry output) utilizing library analysis, analogue design and allosteric site identification.

Picture representing Dr. Halaweish's Research Summary
Picture representing Dr. Halaweish's Research Summary

Current Research Projects

  • Design and synthesis of cancer chemo-therapeutics targeting liver, lung, colon, pancreas, prostate, ovarian and cervical, melanoma, breast cancer and type 2-diabetes.
  • Potential drug candidate targeting kinase and phosphatase inhibitors.
  • Identification of active legend for molecular target such kinase inhibitors, HsP90, NOs inhibitor) through molecular docking and affinity studies (CADD).
  • Bioassay-guided separation, structure elucidation, synthesis and biotransformation of potential drug candidates.
  • Drug Development and nutraceutical standardization of Native Americans medicine.
Cucurbitacins Inspired Organic Synthesis: Potential dual inhibitors targeting EGFR – MAPK pathway
Cucurbitacins Inspired Organic Synthesis: Potential dual inhibitors targeting EGFR – MAPK pathway.
Design and synthesis of a novel series of nitric oxide donating Cucurbitacin Inspired Estrone Analogs (NO-CIEAs).

Design and synthesis of a novel series of nitric oxide donating Cucurbitacin Inspired Estrone Analogs (NO-CIEAs).

Resources

State of the-art NMR and MS facilities, biological screening (in vitro) and animal facilities, genomic and proteomic facilities. Computational and drug design resources.

Teaching

  • Advanced Organic Chemistry (Chemistry 701).
  • Structural determination of Organic Compounds Spectroscopy (Chemistry 724).
  • Molecular Modeling and Drug design (Chemistry 691).
  • Natural products Synthesis (Chemistry 722).
  • Organic Chemistry (Chemistry 326 and 328).

Recent Publications

  1. Novel Mechanistic Insight into the Anticancer Activity of Cucurbitacin D against Pancreatic Cancer (Cucurbitacin D Attenuates Pancreatic Cancer). Cells 2020, 9, 103.
    1. M. Sikander, S. Malik, S. Khan, S. Kumari, N. Chauhan, P. Khan, F. T. Halaweish, B. Chauhan, M. M. Yallapu, M. Jaggi, S. C. Chauhan
  2. "Design, synthesis and biological study of hybrid drug candidates of nitric oxide releasing cucurbitacin-inspired estrone analogs for treatment of hepatocellular carcinoma." Bioorganic Chemistry” 85, 515-533, 2019.
    1. Mahrous A. Abou-Salim, Mohamed A. Shaaban, Mohammed K. Abd El Hameid, Yaseen AMM Elshaier, Fathi Halaweish
  3. "Cucurbitacins inspired organic synthesis: Potential dual inhibitors targeting EGFR–MAPK pathway." European Journal of Medicinal Chemistry 173, 294-304, 2019.
    1. Mater Mahnashi, Sara M. Elgazwi, Mahmoud Salama Ahmed, Fathi T. Halaweish
  4. "Cucurbitacin d reprograms glucose metabolic network in prostate cancer." Cancers 11, 364, 2019.
    1. Mohammed Sikander, Shabnam Malik, Neeraj Chauhan, Parvez Khan, Sonam Kumari, Vivek Kumar Kashyap, Sheema Khan et al
  5. "Isolation of anticancer constituents from Cucumis prophetarum var. prophetarum through bioassay-guided fractionation." BMC complementary and alternative medicine 18, 274-, 2018.
    1. Abdulrhman Alsayari, Lucas Kopel, Mahmoud Salama Ahmed, Hesham S. M. Soliman, Sivakumar Annadurai, Fathi T. Halaweish
  6. "The role of cucurbitacins in combating cancers: A mechanistic review." Pharmacognosy Reviews, 42,157-165, 2018.
    1. Abdulrhman Alsayari, Fathi Halaweish, Narasimman Gurusamy
  7. Cucurbitacin B Restored Cisplatin Sensitivity of Ovarian Cancer Cells by altering Fatty Acid Synthase and LRP-130 Protein Expression, CPQ Cancer, 1(4) 2018.
    1. F. El-Senduny, F. Badria, A. El-Waseef, S. Chauhan, F. Halaweish
  8. Novel series of 6-(2-substitutedacetamido)-4-anilinoquinazolines as EGFR-ERK signal transduction inhibitors in MCF-7 breast cancer cells; European Journal of Medicinal Chemistry, 155, 782-796, 2018.
    1. Rania S.M., Wagdy M. Eldehna, Nasser S.M. Ismail, Sara M. Elgazwi, Hazem A. Ghabbour, Mahmoud Salama Ahmed, Fathi T. Halaweish, Dalal A. Abou El Ella
  9. Ormeloxifene Suppresses Prostate Tumor Growth and Metastatic Phenotypes via Inhibition of Oncogenic β-catenin Signaling and EMT Progression; Molecular Cancer Therapeutics, 16, 2267-2280, 2017.
    1. Bilal Bin Hafeez, Aditya Ganju, Mohammed Sikander, Vivek K. Kashyap, Zubair Bin Hafeez, Neeraj Chauhan, Shabnam Malik, Andrew E. Massey, Manish K. Tripathi, Fathi T. Halaweish, Nadeem Zafar, Man M. Singh, Murali M. Yallapu, Subhash C. Chauhan, Meena Jaggi
  10. Design and synthesis of pyrazolo [3, 4-d] pyrimidines: Nitric oxide releasing compounds targeting hepatocellular carcinoma, Bioorganic and Medicinal Chemistry, 25, 2956-2970, 2017.
    1. Yaseen A. M. M. Elshaier, Mohamed A. Shaaban, Mohammed K. Abd El Hamid, Mostafa H. Abdelrahman, Mahrous A. Abou-Salim, Sara M. Elgazwi, Fathi Halaweish
  11. Biological Screening of Cucurbitacin Inspired Estrone Analogs Targeting Mitogen Activated Protein Kinase (MAPK) Pathway, Chemistry, Biology and Drug Design, 90, 478-484, 2017.
    1. M. S. Ahmed, F. El-Senduny, J. Taylor, F. Halaweish
  12. Mechanistic investigation of hepato-protective potential for cucurbitacins, Med Chem Res 26,1567, 2017.
    1. H. M. Arjaibi, M. S. Ahmed, F. T. Halaweish
  13. Design, Synthesis and Biological Evaluation of Steroidal Analogs as estrogenic / anti-estrogenic agents, Steroids, 118, 32–40, 2017.
    1. A. Alsayari, L. Kopel, M. S. Ahmed, A. Pay, T. Carlson, F. Halaweish
  14. Cucurbitacin D exhibits potent anti-cancer activity in cervical cancer, Scientific Reports, 6, 2016.
    1. M. Sikander, B. Bin Hafeez, S. Malik, A. Alsayari, F. Halaweish, M. Yallapua, C. Subhash, S. Chauhan, M. Jaggi
  15. Assessment of Chemopreventive Contents of Native American Juneberries (Amelanchieralnifolia (Nutt.) Nutt. ex M. Roem.), Pharmaceutical crops,10, 13-21, 2016.
    1. Shimara Gunawardana, Keeli Eberhart, Kerry Hartman1, Fathi T. Halaweish
  16. Approach for chemosensitization of cisplatin-resistant ovarian cancer by cucurbitacin B, Tumor Biology,  37, 685–698, 2016.
    1. F. El-Senduny, F. Badria, A. EL-Waseef, S. Chauhan and F. Halaweish
  17. Nanoparticle formulation of ormeloxifene for pancreatic cancer, Biomaterials, 53, 731-743, 2015.
    1. P. Balabathula, A. Swathi, N. Zafar, P. Thompson, R. T. Ellis, F. Halaweish, S. Chauhan, M. Jaggi, Sheem Khan
  18. Cucurbitacin D is a disruptor of the hsp90 chaperone machinery, Journal of Natural Products, J. Nat. Prod., March 10, 2015.
    1. J. Hall, N. Rice, I. Kopel, F. Halaweish, B. Blagg
  19. Ormeloxifene efficiently inhibits ovarian cancer growth, Cancer Letters, 356, 606–612, 2015.
    1. Diane M. Maher, Sheema Khan, Jordan L. Nordquist, Mara C. Ebeling, Nichole A. Bauer, Lucas Kopel, Man Mohan Singh, Fathi Halaweish, Maria C. Bell, Meena Jaggi, Subhash C. Chauhan
  20. Structural Optimization and Biological Screening of a Steroidal Scaffold Possessing Cucurbitacin-Like Functionalities as B-Raf Inhibitors, ChemMedChem, 9, 1361-1369, 2014.
    1. Mahmoud S. Ahmed, Lucas C. Kopel, Fathi Halaweish
  21. Design, Synthesis and In vitro Anti-tumor Evaluation of Novel Acrylohydrazide Thioglycosides; Med. Chem. 4, 400-406, 2014.
    1. Galal H. Elgemeie, Nahed M. Fathy, Ayman B. Farag, Ossama M. El-Badry, Ghaneia S. Hassan, Kamelia M Amin, Fathi Halaweish