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Fathi Halaweish

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

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

Recent Publications

  1. Sikander, M.; Malik, S.; Khan, S.; Kumari, S.; Chauhan, N.; Khan, P.; Halaweish, F.T.; Chauhan, B.; Yallapu, M.M.; Jaggi, M.; Chauhan, S.C. Novel Mechanistic Insight into the Anticancer Activity of Cucurbitacin D against Pancreatic Cancer (Cuc D Attenuates Pancreatic Cancer). Cells 20209, 103.
  2. Abou-Salim, Mahrous A., Mohamed A. Shaaban, Mohammed K. Abd El Hameid, Yaseen AMM Elshaier, and Fathi Halaweish. "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
  3. Mahnashi, Mater, Sara M. Elgazwi, Mahmoud Salama Ahmed, and Fathi T. Halaweish. "Cucurbitacins inspired organic synthesis: Potential dual inhibitors targeting EGFR–MAPK pathway." European journal of medicinal chemistry 173, 294-304, 2019
  4. Sikander, Mohammed, Shabnam Malik, Neeraj Chauhan, Parvez Khan, Sonam Kumari, Vivek Kumar Kashyap, Sheema Khan et al. "Cucurbitacin d reprograms glucose metabolic network in prostate cancer." Cancers 11, 364, 2019
  5. Alsayari, Abdulrhman, Lucas Kopel, Mahmoud Salama Ahmed, Hesham SM Soliman, Sivakumar Annadurai, and Fathi T. Halaweish. "Isolation of anticancer constituents from Cucumis prophetarum var. prophetarum through bioassay-guided fractionation." BMC complementary and alternative medicine 18, 274-, 2018
  6. Alsayari, Abdulrhman, Fathi Halaweish, and Narasimman Gurusamy. "The role of cucurbitacins in combating cancers: A mechanistic review." Pharmacognosy Reviews, 42,157-165, 2018.
  7. ElSenduny, F., Badria, F., A., EL-Waseef, Chauhan, S. and Halaweish, F., Cucurbitacin B Restored Cisplatin Sensitivity of Ovarian Cancer Cells by altering Fatty Acid Synthase and LRP-130 Protein Expression, CPQ Cancer, 1(4) 2018.
  8. 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; 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.
  9. 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 and Meena Jaggi; 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.
  10. 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, Design and synthesis of pyrazolo[3,4-d]pyrimidines: Nitric oxide releasing compounds targeting hepatocellular carcinoma, Bioorganic & Medicinal Chemistry, 25, 2956-2970, 2017
  11. Ahmed,M.S.; El-Senduny, F.; Taylor, J.; and Halaweish, F.; Biological Screening of Cucurbitacin Inspired Estrone Analogs Targeting Mitogen Activated Protein Kinase (MAPK) Pathway, Chem. Biol & Drug Design, 90, 478-484, 2017.
  12. Arjaibi, H.M., Ahmed, M.S. & Halaweish, F.T. Mechanistic investigation of hepato-protective potential for cucurbitacins, Med Chem Res 26,1567, 2017.
  13. Alsayari, A., Kopel, L., Ahmed, M.S., Pay, A., Carlson, T., and Halaweish, F. Design, Synthesis, and Biological Evaluation of Steroidal Analogs as estrogenic / anti-estrogenic agents, Steroids, 118,32–40, 2017
  14.  Sikander, M., Bin Hafeez, B., Malik, S., Alsayari, A., Halaweish, F., Yallapua, M.  Subhash C. Chauhan, S.,   Jaggi, M., Cucurbitacin D exhibits potent anti-cancer activity in cervical cancer, Scientific Reports, 6, 2016.
  15. Shimara Gunawardana, Keeli Eberhart, Kerry Hartman1, and Fathi T. Halaweish, Assessment of Chemopreventive Contents of Native American Juneberries (Amelanchieralnifolia (Nutt.) Nutt. ex M. Roem.), Pharmaceutical crops,10, 13-21, 2016.
  16. ElSenduny, F., Badria, F., A., EL-Waseef, Chauhan, S. and Halaweish, F., Approach for chemosensitization of cisplatin-resistant ovarian cancer by cucurbitacin B, Tumor Biology,  37, 685–698, 2016.
  17. Balabathula, P.; Swathi A.; Zafar, N.; Thompson, P.; Ellis, R. T.; Halaweish, F.; Chauhan, S., JAGGI, M; Khan, Sheema S.; Chauhan, N., Nanoparticle formulation of ormeloxifene for pancreatic cancer, Biomaterials, 53, 731-743, 2015
  18. Hall, J.; Rice, N.; kopel, l.; Halaweish, F.; Blagg, B., Cucurbitacin D is a disruptor of the hsp90 chaperone machinery, Journal of Natural Products, J. Nat. Prod., March 10, 2015.
  19. 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; Ormeloxifene efficiently inhibits ovarian cancer growth, Cancer Letters, 356, 606–612, 2015
  20. Mahmoud S. Ahmed, Lucas C. Kopel, and Fathi Halaweish, Structural Optimization and Biological Screening of a Steroidal Scaffold Possessing Cucurbitacin-Like Functionalities as B-Raf Inhibitors, ChemMedChem, 9, 1361-1369, 2014.
  21. Galal H. Elgemeie, Nahed M. Fathy, Ayman B. Farag, Ossama M. El-Badry, Ghaneia S. Hassan, Kamelia M Amin and Fathi Halaweish, Design, Synthesis and In vitro Anti-tumor Evaluation of Novel Acrylohydrazide Thioglycosides; Med. Chem. 4, 400-406, 2014