PROF.DR. MEHMET ERDEM BÜYÜKBİNGÖL    
Name : MEHMET ERDEM
Surname : BÜYÜKBİNGÖL
E-Mail : erdem@pharmacy.ankara.edu.tr, ebuyukbingol@gmail.com
Phone Number : +90 312-2033-067
Title : PROF.DR.
Unit : FACULTY OF PHARMACY
Department : Pharmaceutical Chemistry
Personal Information
RESEARCH INTEREST

Our research is mostly focused on structure-based drug design of novel antioxidant molecules bearing indole/benzimidazole moieties along with molecular modeling and synthetic medicinal chemistry. Targeted therapeutic areas of research include genetic-oriented diseases such as cancer, diabetes and neurological disorders i.e. Alzheimer’s disease.

We believe that free radicals play important roles to triggering the incidence of such diseases and also to cause them depending on the environmental circumtendencies. Mammalian cells need to protect themselves constantly against oxgyen-derived free radicals. Upon receiving stress stimuli, the accumulation of reactive oxygen species (ROS) is incerased to cause several diseases including above-mentioned ones by damaging membranes, proteins and DNA. DNA damage generated by oxygen-derived free radicals is related to mutagenesis, carcinogenesis and aging. One of the well-known strategy in cytoprotection (antiaging) by utilizing antioxidant pathways is the synthesis of compounds that mimic antioxidant enzyme activities and/or scavenging the free radicals.

Therefore, we have developed small compounds of melatonin and lipoic acid derivatives for effective antioxidant compounds. Other areas of our drug discovery studies revolve around aldose reductase enzyme inhibition (to prevent or treat diabetes complications such as cataract formation, retinopathy) and retinoids that may also be integrated to the free radical scavenging mechanisms to regulate and/or treat the disease states mentioned above.

Clinically, natural retinoids such as all trans-retinoic acid (ATRA) and retinol (vitamin A) are used in the treatment of proliferative dermatological diseases and in the prevention of certain tumors. However, the
applicability of retinoid remedy is limited due to toxic effects of natural retinoids. Therefore, new retinoidal compounds that comprise specific acting properties on eliminating the reactive oxygen species, together with the lower toxic and/or side effects, could be useful for the precise treatment of above mentioned diseases, clinically. Our group also involved in design, synthesis and cancer cell line studies of certain benzimidazole retinoids which are structurally hybrid compounds between retinoic acid and indole/benzimidazole moieties.

PUBLICATIONS


BOOK CHAPTER:

1. A. Selen GURKAN, Erdem BUYUKBINGOL, Novel Indole Lipoic Acid Derivatives and Their Antioxidant Effects, in Lipoic Acid: Energy Production, Antioxidant Activity and Health Effects, Series: Oxidative Stress and Diseases, Vol: 24, Eds. Mulchand S. Patel and Lester Packer, CRC Press, New York, 2008.



SELECTED PUBLICATIONS:

  1. Gilles KLOPMAN., Erdem BUYUKBINGOL., "An Artificial Intelligence Approach to the Study of the Structural Moieties Relevant to Drug-Receptor Interactions in Aldose Reductase Inhibitors", Molecular Pharmacology, 34, 852-862 (1988).
  2. MesudeY. ISCAN., Erdem BUYUKBINGOL., Mumtaz ISCAN., Fethi SAHIN., Cihat SAFAK., "Effects of 2-Arylbenzimidazoles on the Rat Hepatic Microsomal Monooxygenase System", Comp. Biochem. and Physiol., 92C, 109-115 (1989).
  3. Erdem BUYUKBINGOL., Gilles KLOPMAN., "A New Proposed Model of Aldose Reductase Enzyme Inhibition on the Basis of an Artificial Intelligence Approach: A Computer Automated Structure Evaluation (CASE) Study", J. Math. Chem., 8, 195-205 (1991).
  4. Erdem BUYUKBINGOL., Net DAS., Gilles KLOPMAN., "Design and Synthesis of 1,4-Dihydro-4-oxoquinoline-3-carboxylic acid Derivatives as Inhibitors of Rat Lens Aldose Reductase Enzyme", Archive der Pharmazie, 327, 129-131 (1994).
  5. Erdem BUYUKBINGOL., Sibel SUZEN , Gilles. KLOPMAN, "Studies on the Synthesis and Structure-Activity Relationships of 5-(3'-Indolal)-2-thio- hydantoin Derivatives as Aldose Reductase Enzyme Inhibitors", Farmaco, 49, 443-447 (1994).
  6. Erdem BUYUKBINGOL, Gilles KLOPMAN, "A Novel Aldose Reductase Enzyme Inhibitor, Spirohydantoinylisatin-1-acetic Acid Derivative", Farmaco, 50, 889-891 (1995).
  7. Zeynep ATES, Benay CAN-EKE, Sibel SUZEN, Mumtaz ISCAN and Erdem BUYUKBINGOL, "Effects of a Benzimidazole Compound on Monooxygenase Activities", Farmaco, 52, 703-706 (1997).
  8. Oya BOZDAG, B. GUMUSEL, Rumeysa DEMIRDAMAR, Erdem BUYUKBINGOL, Y. ROLLAND, Rahmiye ERTAN, "Synthesis of Some Novel Oxime Ether Derivatives And Their Activity in the Behavioral Despair Test", Eur. J. Med. Chem., 33, 133-141 (1998).
  9. Benay CAN-EKE, M.Orhan PUSKULLU, Erdem BUYUKBINGOL, Mumtaz ISCAN, "A Study on the Antioxidant Capacities of Some Benzimidazoles in Rat Tissues", Chemico.-Biologico. Int., 113, 65-77 (1998).
  10. Net DAS-EVCIMEN, Bilgehan PEKINER, Sibel SUZEN, Erdem BUYUKBINGOL, "The Inhibitory Effect of Benzodiazepine Derivatives on the Bovine Lens Aldose Reductase Enzyme", Biochem. Mol. Biol. Int., 45, 381-387 (1998).
  11. Sibel SUZEN, Erdem BUYUKBINGOL, "Evaluation of Anti-HIV Activity of 5-(2-Phenyl-3'-indolal)-2-thiohydantoin", Farmaco, 53, 525-527 (1998).
  12. Oya BOZDAG-DUNDAR, Burak DUNDAR, Erdem BUYUKBINGOL, Mino R. CAIRA, 3-Ethyl-5-(5, 6, 7, 8)-tetrahydro-5, 5, 8, 8-tetramethyl-2-naphthylmethyl, Acta Cryst. C55, 1027-1029 (1999).
  13. Meral TUNCBILEK, Oya BOZDAG, Gulgun AYHAN-KILCIGIL, Nurten ALTANLAR, Erdem BUYUKBINGOL, Rahmiye ERTAN, Synthesis And Antimicrobial Activity of Some New Flavonyl Oxime Ether Derivatives, Arzneim.-Forsch./Drug Res., 49, 853-857 (1999).
  14. Sibel SUZEN, Erdem BUYUKBINGOL, "Anti-cancer Activity Studies of Indolalthiohydantoin (PIT) on Certain Cancer Cell Lines", Farmaco, 55, 246-248 (2000).
  15. Sibel SUZEN, Zeynep ATES-ALAGOZ, Erdem BUYUKBINGOL, Mino R. CAIRA, Synthesis and structure of 2-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalene)]-5-benzimidazole ethylcarboxylate monohydrate, J. Chem. Crystallogr., 30, 103-107 (2000).
  16. Engin KENDI, Zeynep ATES-ALAGOZ, Sibel SUZEN, Erdem BUYUKBINGOL, Crystal Structure of 2-[(5, 6, 7, 8-tetrahydro-5, 5, 8, 8-tetramethyl)-2-naphthyl]-1-ethyl-1H-benzimidazole-5-carboxylic acid ethyl ester, Analytical Sciences, 17, 567-568 (2001).
  17. Zeynep ATES-ALAGOZ, Erdem BUYUKBINGOL, "Synthesis of Some New Tetrahydronapthalene Benzimidazole Derivatives", Heterocyclic Communications, 7, 455-461 (2001).
  18. Burak DUNDAR, Oya BOZDAG-DUNDAR, Benay CAN-EKE, Tulay COBAN, Mumtaz ISCAN, Erdem BUYUKBINGOL, "Synthesis and Antioxidative Properties of Novel Thiazolidinedione/Imidazolidinedione Compounds as Retinoids", Pharmazie, 57, 438-441 (2002) .
  19. Mino R. CAIRA, Erdem BUYUKBINGOL, Adeboye ADEJARE, William R. MILLINGTON, "Crystal Structure of the Dipeptide Cyclo(Glycyl-L-Glutamine)", Analytical Sciences, 18, 1175-1176 (2002).
  20. Sibel SUZEN, Erdem BUYUKBINGOL, "Recent Studies of Aldose Reductase Enzyme Inhibition for Diabetic Complications", Current Medicinal Chemistry, 10, 1329-1353 (2003) .
  21. Sibel SUZEN, B. Tolga DEMIRCI, Erdem BUYUKBINGOL, Sibel A. OZKAN, "Electrochemical Evaluation and Determination of 5-(3'-indolal)-2-thiohydantoin Derivatives by Voltammetric Studies: Possible Relevance to in vitro Metabolism", New J. Chemistry, 27, 1007-1011 (2003).
  22. Zeynep ATES-ALAGOZ, Benay CAN-EKE, Tulay COBAN, Mumtaz ISCAN, Erdem BUYUKBINGOL, "Antioxidant Properties of Novel Benzimidazole Retinoids", Archive der Pharmazie, 337, 188-92 (2004) .
  23. A. Selen GURKAN, Arzu KARABAY, Zeliha BUYUKBINGOL, Adeboye ADEJARE, Erdem BUYUKBINGOL, Syntheses of Novel Indole Lipoic Acid Derivatives and Their Antioxidant Effects on Lipid Peroxidation”, Archive der Pharmazie, 338, 67-73, (2005) .
  24. Zeynep ATES-ALAGOZ, Zeliha BUYUKBINGOL, Erdem BUYUKBINGOL, “Synthesis and Antioxidant Properties of Some Indole Ethylamine Derivatives as Melatonin Analogs”, Pharmazie, 60, 643-647, (2005) .
  25. Fulya BALABAN, Zeynep ATES-ALAGOZ, Erdem BUYUKBINGOL, Mesude ISCAN, "Genotoxicity Studies on Benzimidazole Retinoids", Pharmazie, 60, 855-862, (2005) .
  26. Zeynep ATES-ALAGOZ, Mehmet ALP, Canan KUS, Sulhiye YILDIZ, Erdem BUYUKBINGOL, Hakan Goker, "Synthesis and Potent Antimicrobial Activities of Some Novel Retinoidal Monocationic Benzimidazoles", Archive der Pharmazie, 339, 74-80 (2006) .
  27. Hande GURER-ORHAN, Hilmi ORHAN, Sibel SUZEN, Orhan PUSKULLU,  Erdem BUYUKBINGOL,Synthesis and evaluation of in vitro antioxidant capacities of some benzimidazole derivatives, J. Enzyme Inhibition Med. Chem., 339, 74-80 (2006).
  28. Zeynep Ates-Alagoz, Tulay Coban, Erdem BUYUKBINGOL, "Synthesis and Antioxidant Activity of New Tetrahydro-Naphthalene-Indole Derivatives as Retinoid and Melatonin Analogs", Archiv der Pharmazie, 339, 193-200 (2006).
  29. Zeynep ATES-ALAGOZ, Sulhiye YILDIZ, Erdem BUYUKBINGOL, “Antimicrobial Activities of Some Tetrahydronaphthalene-Benzimidazole Derivatives”, Chemotherapy, 53, 110-113 (2007).
  30. Erdem BUYUKBINGOL, Arzu SISMAN, Murat AKYILDIZ, Ferda Nur ALPARSLAN, Adeboye ADEJARE, Adaptive neuro-fuzzy inference system (ANFIS): A new approach to predictive modeling in QSAR applications: A study of neuro-fuzzy modeling of PCP-based NMDA receptor antagonists, Bioorganic & Medicinal Chemistry, 15, 4265-4282 (2007) .
  31. A Kevser PISKIN, Zeynep ATES-ALAGOZ, F. Belgin ATAC and Erdem BUYUKBINGOL, “DNA Binding and Antiproliferative Effects of Some Benzimidazole Retinoids”, Turk. J. Biochem, 34 (1), 39-43 (2009).
  32. Zeynep-ATES-ALAGOZ, Nurten ALTANLAR, Erdem BUYUKBINGOL, Synthesis and Antimicrobial Activity of New Tetrahydro-Naphthalene-Thiazolidinedione and Thiohydantoine Derivatives, J. Heterocyclic Chem., 46, 1375-1379 (2009).
  33. Ozlem ERDAS, Erdem BUYUKBINGOL, Ferda Nur ALPARSLAN, Adeboye ADEJARE, Modeling and Predicting Binding Affinity of Phencyclidine-Like Compounds Using Machine Learning Methods, J. Chemometrics, 24, 1-13 (2010).
  34. A. Selen GURKAN, Arzu KARABAY, Zeliha BUYUKBINGOL, Erdem BUYUKBINGOL, Synthesis And Effects Of Some Novel Tetrahydronaphthalene Derivatives On Proliferation And Nitric Oxide Production In Lipopolysaccharide Activated Raw264.7 Macrophages, Eur. J. Med. Chem., 46, 468-479 (2011).
  35. A. Selen Gurkan-Alp, Mine Mumcuoglu, Cenk A. Andac, Emre Dayanc, Rengul Cetin-Atalay, Erdem Buyukbingol, Synthesis, anticancer activities and molecular modeling studies of novel indole retinoid derivatives, Eur. J. Med. Chem., 58, 346-354 (2012).
  36. ERDAS, Ozlem, ANDAC, Cenk, A., GURKAN-ALP, Selen, ALPARSLAN, Ferda, BUYUKBINGOL, Erdem, Compressed Images for Affinity Prediction (CIFAP): A Study on Predicting Binding Affinities for Checkpoint Kinase 1 Protein Inhibitors, J. Chemometrics, Accepted for publication, 2013.
  37. ELMAZOGLU, Zubeyir, GURKAN-ALP, A. Selen, ANDAC, A. Cenk, DURMAZ, Irem, ATALAY, Rengul, BUYUKBINGOL, Erdem, Synthesis and anticancer activities of some novel farnesylthiosalicylamide / farnesylanthranilamide derivatives, Eur. J. Med. Chem., Submitted for publication, 2013.
  38. DEMIRCI, Asli, GURKAN-ALP, A. Selen, ANDAC, A. Cenk, YILDIRIM, C. Deniz, CETIN-ATALAY, Rengul,  BUYUKBINGOL, Erdem,   Synthesis and anticancer activities and molecular modeling studies of some novel 4-trans,trans-farnesylthiobenzamide and 3-trans,trans-farnesylthiobenzamide derivatives, in preperation, 2013.