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Hesham Fahmy

Hesham Fahmy

Title

Associate Professor

Office Building

Avera Health and Science Center

Office

269

Mailing Address

Avera Health & Science 269
Pharmaceutical Sciences-Box 2202C
University Station
Brookings, SD 57007

Education

Ph.D. Medicinal Chemistry
M.S. Pharmaceutical Chemistry
B. S. Pharmacy

Academic Interests

Medicinal Chemistry
Drug design
Synthetic Organic Chemistry
Natural Products

Academic Responsibilities

Medicinal Chemistry I (PHA 340)
Medicinal Chemistry II (PHA 341)
Advanced Concepts in Medicinal Chemistry (PHA 840)
Techniques in Pharmaceutical Sciences (PHA 846)

Committee Activities

Pharm D hooding and commencement committee
Curricular progression and variation committee
University Stewardship and sustainability committee

Area(s) of Research

Design & synthesis of Coricotropin-releasing factor (CRF) receptor antagonists
Design & synthesis of T-/L-types calcium channel blockers
Semi-synthetic natural products of medicinal interest
Skin cancer chemoprevention
Marine natural products of medicinal interest

List of PUBLICATIONS:
I- PAPERS:

1- Synthesis of 2-imino and 2-hydrazono thiazolo[4,5-d]pyrimidines as corticotropin releasing factor (CRF) antagonists: Mohamed Teleb, Katerina Spyridaki, George Liapakis, Hesham Fahmy. European Journal of Medicinal Chemistry, 138, 900-908 (2017)

2- Synthesis of Novel N3-substituted Dihydropyrimidine Derivatives as L-/T- Type Calcium Channel Blockers, Mohamed Teleb, Fang-Xiong Zhang, Ahmed M. Farghaly, Omaima M. Aboul Wafa, Frank R. Fronczek, Gerald W. Zamponi and Hesham Fahmy. European Journal of Medicinal Chemistry 134, 52-61 (2017)

3- Synthesis and Biological Evaluation of Novel N3-substituted Dihydropyrimidine Derivatives as T-Type Calcium Channel Blockers and Their Efficacy as Analgesics in Mouse Models of Inflammatory Pain, Mohamed Teleb, Fang-Xiong Zhang, Junting Huang, Vinicius M Gadotti, Ahmed M. Farghaly, Omaima M. AboulWafa, Gerald W. Zamponi and Hesham Fahmy. Bioorganic & Medicinal Chemistry 25, 1926-1938 (2017)

4- A comprehensive review in development of thiazolo[5,4-d]pyrimidines based molecules in medicinal chemistry, Bhimanna Kuppast, Mohamed Teleb, Hesham Fahmy, Jacob Journal of Medicinal Chemistry, 2(1), 008 (2017)

5- Structure and Function of Small Non-Peptide CRF Antagonists and their Potential Clinical Use, Fahmy, H., Kuppast, B., Ismail, M.; Current Molecular Pharmacology: In press. Available ahead of print at: http://benthamscience.com/journals/current-molecular-pharmacology (2017)

6- Thiazolo[4,5-d]pyrimidines as a privileged scaffold in drug discovery. Kuppast, B. and Fahmy, H.: European Journal of Medicinal Chemistry, 113, 198-213 (2016)

7- Synthesis of New Thiazolo[4,5-d]pyrimidines as Corticotropin Releasing Factor Modulators. Kuppast, B., Spyridaki, K., Lynch, C., Hu, Y., Liapakis, G., Davies, G., Fahmy, H., Medicinal Chemistry, 11, 50-59 (2015).

8- Evaluation of the anti-melanoma activities of (1S,2E,4R,6E,8R,11S,12R)-8,12-epoxy-2,6-cembradiene-4,11-diol, (1S,2E,4R,6E,8S,11R,12S)-8,11-epoxy-4,12-epoxy-2,6-cembradiene and (1S,4R,13S)-cembra-2E,7E,11E-trien-4,13-diol from the Red Sea soft coral Sarcophyton glaucum.Szymanski, P., Ahmed, S., Radwan, M., Khalifa, S., and Fahmy, H., Natural Products Communication, 9(8), 1143-1146 (2014).

9- Evaluation of the anti-melanoma activities of Sarcophine, (+)-7α,8β Dihydroxydeepoxy sarcophine and Sarcophytolide from the Red Sea soft coral Sarcophyton glaucum. Szymanski, P. T., Ahmed, S. A., Radwan, M. M., Khalifa, S. I., and Fahmy, H.: Natural Products Communication, 9 (2), 151-154 (2014)

10- Synthesis of new substituted pyrimidines as corticotropin releasing factor (CRF) receptor ligands. Kuppast, B., Spyridaki, K., Liapakis, G. Fahmy, H., European Journal of Medicinal Chemistry, 78, 1-9 (2014)

11- Chemopreventive Effect of Sarcophine-diol on NOR-1-Induced TPA-Promoted Skin Carcinogenesis in Female HOS:HR-1 Mice. Szymanski, P. T., Ahmed, S. A., Khalifa, S., Tokuda, H., Ichiishi, E., Iida, A., Suzuki, N. and Fahmy, H.: Natural Products Communication, 8 (2), 153-154 (2013)

12- Bioactive cembranoids from the Red Sea soft coral Sarcophyton glaucum. Abou El-Ezz, R. F., Ahmed,S. A., Radwan, M. M., Ayoub, N. A., Afifi, M. S., Ross, S. A., Szymanski, P., Fahmy, H., Khalifa, S. I.: Tetrahedron Letters, 54, 989-992 (2013)

13- Chemopreventive effects of combination of honokiol and magnolol with alpha- santalol on skin cancer development. Chilampalli, C.; Zhang, X.; Kaushik, R. S.; Young, A.; Zeman, D.; Hildreth, M. B.; Fahmy, H.; Dwivedi, C.: Drug Discoveries & Therapeutics, 7(3), 109-115 (2013)

14- Sarcophine-Diol Inhibits Expression of COX-2, Inhibits Activity of cPLA2, Enhances Degradation of PLA2 and PLCγ1 and Inhibits Cell Membrane Permeability in Mouse Melanoma B16F10 Cells. Szymanski, P., Muley, P., Ahmed, S., Khalifa, S., Fahmy, H.: Marine Drugs, 10, 2166-2180 (2012).

15- The homeostasis hormone and its CRF1 receptor. From structure to function. Fahmy, H., Spyridaki, K., Kuppast, B., Liapakis, G.: Hormones, 11(3):254-271 (2012).

16- Sarcophine-Diol, a Skin Cancer Chemopreventive Agent, Inhibits Proliferation and Stimulates Apoptosis in Mouse Melanoma B16F10 Cell Line. Szymanski, T., Kuppast, B., Ahmed, A., Khalifa, S., Fahmy, H.: Marine Drugs, 10, 1-19 (2012).

17- Dose-response on the chemopreventic effects of sarcophine-diol on UVB-induced skin tumor development in SKH-1 hairless mice. Guillermo, R.F., Zhang, X., Kaushik, R.S., Zeman, D., Ahmed, S., Khalifa, S., Fahmy, H., Dwivedi, C.: Marine Drugs, 10, 2111-2125 (2012).

18- Time and dose-response effects of honokiol on UVB-induced skin cancer development. Guillermo, R.F., Chilampalli, C., Zhang, X., Zeman, D., Fahmy, H., and Dwivedi, C.: Drug Discoveries and Therapeutics, 6:140-146 (2012).

19- Chemopreventive effects of magnolol on UVB-induced skin cancer development in mice and its possible mechanism of action. Chilampalli, C., Guillermo, R., Zhang, X., Kaushik, R.S., Young, A., Zeman, D., Hildreth, M., Fahmy, H., Dwivedi, C.: BMC Cancer, 11:456 (2011).

20- Honokiol, a chemopreventive agent against skin cancer induces cell cycle arrest and apoptosis in human epidermoid A431 cells. Chilampalli, C., Guillermo,R. , Kaushik, R., Young, A., Chandrasekher, G., Fahmy, H., Dwivedi, C.: Experimental Biology and Medicine, 1-9 (2011).

21- Inhibitory effect and transcriptional impact of berberine and evodiamine on human white preadipocyte differentiation. Hu, Y., Fahmy, H., Zjawiony, J., Davies, G.: Fitoterapia, 81(4), 259-268 (2010).

22- Alpha-santalol, a chemopreventive agent against skin cancer, causes G2/M cell cycle arrest in both p53-mutated human epidermoid carcinoma A431 cells and p53 wild-type human melanoma UACC-62 cells. Zhang X, Chen W, Guillermo R, Chandrasekher G, Kaushik RS, Young A, Fahmy H, Dwivedi C.: BMC Res Notes, 3, 3:22 (2010).

23- Chemopreventive Effects of Honokiol on UVB-induced Skin Cancer Development. Chilampalli, C., Zhang, X., Fahmy, H., Kaushik, R., Zeman, D., Hildreth, M., Dwivedi, C.: Anticancer Research, 30, 777-784 (2010).

24- Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory and antimicrobial agents. Bekhit, A. Fahmy, H., Rostom, S., Bekhit, A. A.: European Journal of Medicinal Chemistry, 45 6027-6038 (2010).

25- Chemopreventive Effects of Sarcophine-diol on Ultraviolet Binduced Skin Tumor Development in SKH-1 Hairless Mice. Zhang, X., Bommareddy, A., Chen, W., Hildreth, M. B., Kaushik, R., Zeman, D., Khalifa, S., Fahmy, H., Dwivedi, C.: Marine Drugs (Impact Factor 3.85), 7, 153-165 (2009).

26- Sarcophine-diol, a chemopreventive agent of skin cancer, inhibits cell growth and induces apoptosis through extrinsic pathway in human epidermoid carcinoma A431 cells. Zhang, X., Bommareddy, A., Chen, W., Khalifa, S., Kaushik, R., Fahmy, H., Dwivedi, C.: Translational Oncology, 2(1), 21-30 (2009).

27- Synthesis of somesulfonamides, disubstituted sulfonylureas or thioureas and some structurally related variants. A class of promising antitumor agents. Faidallah, H.M., Al-Saadi, M. S., Rostom, S. A. F. and Fahmy, H.: Medicinal Chemistry Research, 16, 300-318 (2008).

28- Chemopreventive Effects of Sacrotriol in Ultraviolet B-Induced Skin Tumor Develiopment in SKH-1 Hairless Mice. Kundoor, V., Zhang, X., Bommareddy, A., Khalifa, S., Fahmy, H., Dwevedi, C.: Marine Drugs, 5, 197-207 (2007).

29- Chemopreventive effects of sarcophine-diol on skin tumor development in CD-1 mice. Xiaoying Zhang, Vipra Kundoor, Sherief Khalifa, David Zeman, Hesham Fahmy, Chandradhar Dwivedi, Cancer Letters, 253, (1), 53–59 (2007)

30- Synthesis of Novel Benzofuran and Related Benzimidazole Derivative for Evaluation of in vitro Anti-HIV-1, Anticancer, and Antimicrobial Activities. Rida, S., El-Hawash, S., Fahmy, H., Hazza, A., El-Meligy, M.: Arch Pharm Res, 29(10), 826-833 (2006).

31- A Possible Mechanism of Action of the Chemopreventive Effects of Sarcotriol on Skin Tumor Development in CD-1 Mice. Kundoor, V., Zhang, X., Khalifa, S., Fahmy, H., Dwivedi, C.: Marine Drugs, 4, 274-285 (2006).

32- Potent Skin Cancer Chemopreventive Activity of Some Novel Semi-synthetic Cembranoids from Marine Sources. Fahmy, H., Zjawiony, J., Konoshima, K., Tokuda, H., Khan, S., Khalifa, S.: Marine Drugs, 4, 28-36 (2006).

33- Bioisosteric modification of Salvinorin A, a Potent and Selective Kappa-Opoid Receptor Agonist. Stewart, J., Fahmy, H., Roth, B., Yan, F., Zjawiony, J. Bioisosteric Modification of Arzneim Forsch. Drug Res. 56(4), 269-275 (2006).

34- Synthesis and in vitro Evaluation of Some Novel Benzofuran Derivatives as Potential Anti-HIV-1, Anticancer and Antimicrobial Agents. Rida, S., El-Hawash, S., Fahmy, H., Hazza, A., El-Meligy, M. Acrch Pharm Res., 29(1), 16-25 (2006).

35- An Improved Synthesis of 7,8-Epoxy-1,3,11-cembratriene-15R(α),16-diol,A Cembranoid of Marine Origin With a Potent Cancer Chemopreventive Activity.
Fahmy, H., Khalifa, S. I., Konoshima, T., Zjawiony, J. KMarine Drugs, 1, 1-7 (2004).

36- A Direct Synthesis of 3,5-Dibromo-O-methyl-L-tyrosine. Stewart, J. Katsuyama, I., Fahmy, H., Fronczek, F. R., Zjawiony, J. K.: A Direct Synthetic Communications, 34(3), 531-539 (2004).

37- Design and Synthesis of Some Substituted 1H-pyrazolyl thiazolo[4,5-d]pyrimidines as Anti-inflammatory - Antimicrobial Agents. Bekhit, A. A., Fahmy, H., Rostom, S. A., Baraka, A.: Eur. J. Med. Chem. 38(1), 27-36 (2003).

38- Synthesis and in-vitro Anti-HIV Screening of Certain 2-(benzoxazol-2-ylamino)-3H-4-oxopyrimidines. Rostom, S. A., Fahmy, H., Saudi, M. N.: Scientia Phatmaceutica, 71(2), 57-74 (2003).

39- Synthesis of 2-(4-Biphenylyl)-quinoline-4-carboxylate and carboxamide Analogs. New Human Neurokinin- 3(hNM-3) Receptor Antagonists. Saudi, M. N., Rostom, S. F., Fahmy, H., El Ashmaway, I. M.: Arch. Pham. Pharm. Med. Chem.(Weinheim) 336(3), 165-174 (2003).

40- Synthesis and in-vitro Evaluation of The Anticancer Activity of Novel Fluorinated Thiazolo[4,5-d]pyrimidines. Arch. Pham. Fahmy, H., Rostom, S. A., Saudi, M. N., Zjawiony, J. K., Robins, D. J.: Pharm. Med. Chem. (Weinheim) 336(4-5), 216-225(2003).

41- Design and Synthesis of Some Substituted 1H-Pyrazolyl-Oxazolidines or 1H-Pyrazolyl-Thiazolidines as Anti-inflammatory-Antimicrobial agents. Bekhit, A., Fahmy, H.:Arch. Pham. Pharm. Med. Chem. (Weinheim), 336(2), 111-118 (2003).

42- Synthesis of cis- and trans-7-chloro-7,8,9,10-tetrahydrobenzo[a]pyren-8-ol: Remarkable Solvent Effect on Epoxide Hydrochlorination Diastereoselectivity. Mahindaratne, M., Fahmy, H., Garcia, J. A., Negrete, G. R.: Synthetic Commuincation, 33(8), 1391-1398 (2003).

43- A Semi-synthetic Analog of the Cembranoid Sarcophine. Fahmy, H., Zjawiony, J. K., Khalifa, S., Fronczek, F. R.: Acta Cryst. C59, 85-87 (2003).

44- Semi-synthesis of New Sarcophine Derivatives with Chemopreventive Activity. Katsuyama, I., Fahmy, H., Zjawiony, J. K., Zjaiowny, J. K., Khalifa, S. I., Kilada, R. W, Konoshima, T. , Takasaki, M. and Tokuda, H..: J. Natural Products, 65, 1808-1814 (2002).

45- Synthesis of Some New Bis-thiazoles As Possible Anticancer Agents. Fahmy, H., Bekhit, A. A.: Pharmazie, 57(12), 800-803 (2002).

46- Synthesis and Antitumor Evaluation of New 1-Polysubstituted Thiazole and Derived Thiazolo[4,5-d]pyrimidine Systems. Fahmy, H., Rostom, S. A., Bekhit, A. A.: Arch. Pharm. Pharm. Med. Chem. (Weinheim) 335(5), 213-222 (2002).

47- Synthesis of Some New Triazoles as Potential Antifungal Agents. Fahmy, H.: Bollitino Chemico Pharmaceutico, 140, 423-427 (2001).

48- Synthesis and Antimicrobial Screening of Some Novel Thiazoles, Dithiazoles, and Thiazolylpyridines. Fahmy, H.: Pharmazie, 52(10), 750-753 (1997).

49- Synthesis and Antimicrobial Activity of Rhodanine Derivatives. Habib, N. S., Rida, S. M., Badawey, E. A., Fahmy, H. T., Ghozlan, H. A.: Eur. J. Med. Chem., 32(9), 759-762 (1997).

50- Synthesis and Biological Investigations of Novel Thiazolyl-benzimidazoles and Benzimidazolyl-thiazlo[4,5-d]pyrimidines. Habibi, N. S., Rida, S. M., Badawey, E. A., Fahmy, H. T., Ghozlan, H. A.: Pharmazie, 52(5), 346-350 (1997).

51- Synthesis of Novel Thiazolo[4,5-d]pyrimidines Derivatives for Antimicrobial, Anti-HIV, and Anticancer Investigation. Habib, N. S., Rida, S. M., Badawey, E. A., Fahmy, H. T., Ghozlan, H. A.: Pharmazie, 51(12), 927-931 (1996).

52- Condensed Thiazoles:I. Synthesis of 5,7-Disubstituted Thiazolo[4,5-d]pyrimidines as Possible Anti-HIV, Anticancer, and Antimicrobial Agents. Habib, N. S., Rida, S. M., Badawey, E. A., Fahmy, H.T.: Monatsh Chemie, 127(11), 1203-1207 (1996).

53- Condensed Thiazoles: II. Synthesis of 7-Substituted Thiazolo[4,5-d]pyrimidines as Possible Anti-HIV, Anticancer, and Antimicrobial Agents. Rida, S. M., Habib, N. S., Badawey, E. A., Fahmy, H. T.: Monatsh Chemie, 127(11), 1209-1214 (1996).

54- Synthesis of Some Novel Perhydrotriazepine-3,6-diones of Potential Antifungal Activity. Mahran, M. A., El-Sayed, O. A., Fahmy, H. T., Ashour, F. A.: Alex. J. Pharm. Sci., 10(2), 133-135 (1996).

55- Synthesis and Biological Investigations of Some New Thiazolyl-benzimidazoles and Benzimidazolyl-thiazolo[3,2-a]pyridines. Rida, S. M., Habib, N. S., Badawey, E. A., Fahmy, H. T., Ghozlan, H. A.: Arch. Pharm. (Weinheim), 328(4), 325-328 (1995).

56- Potential Antimicrobials I. Synthesis and Structure-Activity Studies of Some New Thiazolo[4,5-d]pyrimidine Derivatives. Badawey, E. A., Rida, S. M., Hazza, A. A., Fahmy, H. T., Gohar, Y.M.: Eur. J. Med. Chem., 28(2), 91-96 (1993).

57- Potential Antimicrobials II. Synthesis and In-Vitro Anti-Microbial Evaluation of Some New Thiazolo[4,5-d]pyrimidine Derivatives. Badawey, E. A., Rida, S. M., Hazza, A. A., Fahmy, H. T., Gohar, Y.M.: Eur. J. Med. Chem., 28(2), 97-101 (1993).

58- Assessment of Anti-HIVActivity of Some Benzimidazolyl-thiazoles. Badawey, E. A., Hazza, A. A., Rida, S. M., Fahmy, H. T.: Arch. Pharm. (Weinheim), 325(9), 565-567 (1992).

II- PATENTS:

59- Salvinorin Derivatives with Selective k-Opioid Receptor Affinity, Zjawiony, J. K., Fahmy, H.; Stewart, J.; Roth, B.: PCT Int. Appl. WO 2006012643, A2 20060202 (2006), C.A. 144, 164284 (2006)

60- Cembranoids of Chemopreventive Activity. Zjawiony, J. K., Fahmy, H., Katsuyama, I., Khalifa, S., Konoshima, T.: PCT Int. Appl. WO 2003095404, A1 20031120 (2003), C.A. 139, 381637 (2003).

Department(s)