Pr. PETER G. GOEKJIAN
Laboratoire de Chimie Organique 2
UMR C.N.R.S.-U.C.B.L. 5246 ICBMS
Université Claude Bernard - Lyon 1
C.P.E. Lyon - Bâtiment 308D
69622 Villeurbanne Cedex
goekjian@univ-lyon1.fr
(33) 04 72 44 8183 (tel.)
(33) 04 78 89 8914(fax)
32e Section
Professeur, 2e Classe
PEDR
DONNEES PERSONNELLES: Bilingue en Français et Anglais. Né en 1963 à Fairfax, VA, USA. Résident à Saint-Jean-Cap-Ferrat, France, 1969-1970; Maisons-Laffitte, France, 1970-1978; Etats Unis 1978-2000 ; Lyon 2000 au présent. Nationalité américaine.
POSTES ACADEMIQUES:
Université Claude Bernard - Lyon 1, Villeurbanne, France. Septembre, 2000 - situation actuelle. Professeur de Chimie, UFR Chimie-Biochimie. Chimie Organique. Directeur de l'équipe Chimie Organique 2-Glycochimie 2001-2008. Recherche: synthèse totale des produits naturels glycosides, méthodologies ciblées, inhibiteurs de protéines kinases, rôle de la glycosylation dans l'expression des gènes.
Mississippi State University, Mississippi State, MS, USA. Juillet, 1994 - Aout 2000. Assistant Professor, Département de Chimie. Organic Chemistry. Recherche: chimie organique synthétique, base structurale de l'activité biologique, synthèse électrochimique.
STAGES POSTDOCTORALES:
University of Wisconsin, Madison, WI. Septembre 1991 - Juin 1994. Stage Postdoctoral avec le Pr. Edwin Vedejs. Total synthesis of the pyrrolizidine alkaloid seco-base Otonecine.
Harvard University, Cambridge, MA. Janvier - Juin 1991. Stage Postdoctoral avec le Pr. Yoshito Kishi. The Conformational Analysis of C-Glycosides.
EDUCATION:
Harvard University, Cambridge, MA. Septembre 1984 - Janvier 1991. Ph.D. en Chimie Organique. Directeur de thèse: Prof. Yoshito Kishi.The Conformational Analysis of C-Glycosides: An Experimental Approach to Carbohydrate Conformation.
Haverford College, Haverford PA. Septembre 1980 - Juin 1984. B.A. en Chimie.
STAGE EN RECHERCHE INDUSTRIELLE:
E.I. DuPont de Nemours, Experimental Research Station, Central Research and Development, Wilmington, Delaware. Juin - Aout 1984. Synthesis of a suicide substrate inhibitor of cholesterol biosynthesis.
PUBLICATIONS :
1. Caroline Corbel, Rose Haddoub, Damien Guiffant, David Gueyrard, Jérôme Lemoine, Morgane Ratin, Laurent Meijer, Stephane Bach and Peter Goekjian. "Identification of potential cellular targets of aloisine A by affinity chromatography" Bioorganic and Medicinal Chemistry 2009, 17(15), 5572-5582
2. Cédric Schneider, David Gueyrard, Benoît Joseph and Peter G. Goekjian. "Chemoselective Functionalization of α-Carbolines at 2-, 3-, 4- and 6-positions by Suzuki-Miyaura Reactions" Tetrahedron 2009, 65(27), 5427-5437.
3. Rose Haddoub, David Gueyrard and Peter G. Goekjian. "Synthesis of C-linked immobilized analogs of Aloisine A by ‘click' chemistry" Tetrahedron Letters 2009, 50, 741-744.
4. Mazen Sleiman, Jean-Manuel Raimundo, Annabelle Varrot, Peter G. Goekjian and Marc Gingras."Glycosylated asterisks are among the most potent low valency inducers of Concanavalin A aggregation" Chemical Communications, 2008, 6507-6509.
5. Shaheen Ahmed, Carlo Gambacorti-Passerini, Pierre Garcia, Peter Goekjian, David Goyard, David Gueyrard, Benoit Joseph, Luca Moligny, Florence Popowycz, Leonardo Scapozza and Cedric Schneider. "Antiproliferative a-Carbolines And Therapeutic Uses Thereof". European patent application EP 08015802.5, filed September 8, 2008.
6. Shaheen Ahmed, Carlo Gambacorti-Passerini, Peter Goekjian, David Gueyrard, Rosalind Gunby, Florence Popowycz, Leonardo Scapozza, Cedric Schneider and Alfonso Zambon. "Antiproliferative Compounds And Therapeutic Uses Thereof". European patent application EP 08 006651.7, filed March 31, 2008.
7. Philippe Belmont, Laurent Meijer, Philip Cohen, Amaury Patin, Johann Bosson, and Peter Goekjian, "Dérivés de tétrahydrocyclopenta[c]acridines inhibiteurs de kinases et leurs applications biologiques" European patent application 08 00275, filed January 18, 2008.
8. Carole Lamy, Jérôme Lemoine, Denis Bouchu, Peter Goekjian and Peter Strazewski. "Control over the Histidine-Glycine Ratio in Random Copolymers Generated from Aqueous Solutions of the Amino Acids, Carbonyldiimidazole and Chlorotrimethylsilane through Pulsed Addition of the Glycine Precursor into Polymerizing Histidine," ChemBioChem 2008, 9, 710 - 713.
9. Marie-Aude Hiebel, Béatrice Pelotier, Peter Goekjian and Olivier Piva. "2,6-Disubstituted Tetrahydropyrans by Tandem Cross-Metathesis-Iodocyclisation." Eur. J. Org. Chem. 2008, 713-720.
10. Matthieu Corbet, Benjamin Bourdon, David Gueyrard and Peter G. Goekjian. "A Julia olefination approach to the synthesis of functionalized enol ethers and their transformation into carbohydrate-derived spiroketals," Tetrahedron Letters 2008, 49(5), 750-754.
11. Benjamin Bourdon , Matthieu Corbet, Patrice Fontaine Peter G. Goekjian and David Gueyrard. "Synthesis of enol ethers via a Julia modified olefination of lactones: application to the preparation of tri- and tetrasubstituted exoglycals," Tetrahedron Letters 2008, 49(5), 747-749.
12. Kaïss Aouadi, Bénédicte Defaut, Peter G. Goekjian and David Gueyrard. "Synthesis of semicyclic dienes derived carbohydrate by Julia olefination on anomeric vinyl sulfones," Synlett 2007, (16), 2590-2592.
13. Carole Lamy, Johann Hofmann, Hélène Parrot-Lopez, and Peter Goekjian. "Synthesis of a fluoroalkene peptidomimetic precursor of N-acetyl-L-glutamyl-L-alanine," Tetrahedron Lett.2007, 48(35), 6177-6180.
14. Schneider, Cédric; Gueyrard, David; Popowycz, Florence; Joseph, Benoît; Goekjian, Peter G. Synthesis of 6-Substituted Pyrido[2,3-b]indoles by Electrophilic Substitution," Synlett 2007, 14, 2237-2241.
15. Anne-Sophie Bretonnet , Anne Jochum, Olivier Walker, Isabelle Krimm, Peter Goekjian , Olivier Marcillat , Jean-Marc Lancelin. "NMR Screening Applied to the Fragment-Based Generation of Inhibitors of Creatine Kinase Exploiting a New Interaction Proximate to the ATP Binding Site", J. Med. Chem. 2007, 50(8); 1865-1875.
16. Johannes Trapp, Anne Jochum, Rene Meier, Laura Saunders, Brett Marshall, Conrad Kunick, Eric Verdin, Peter Goekjian, Wolfgang Sippl, and Manfred Jung. "Adenosine mimetics as inhibitors of NAD + -dependent histone deacetylases - from kinase to sirtuin inhibition", J. Med. Chem. 2006, 49, 7307-7316.
17. Mahmoud Benltifa, Sebastien Vidal, Bernard Fenet, Moncef Msaddek, Peter G. Goekjian, Jean-Pierre Praly, Attila Brunyanszki, Tibor Docsa, Pal Gergely. "In search of glycogen phosphorylase inhibitors: 5-substituted 3-C- glucopyranosyl-1,2,4-oxadiazoles from b -D-glucopyranosyl cyanides upon cyclization of O-acylamidoxime intermediates." Eur. J. Org. Chem. 2006, 18, 4242-4256.
18. Mahmoud Benltifa, Sébastien Vidal, David Gueyrard, Peter G. Goekjian, Moncef Msaddek, and Jean-Pierre Praly. "1,3-Dipolar cycloaddition reactions on carbohydrate-based templates: synthesis of spiro-isoxazolines and 1,2,4-oxadiazoles as glycogen phosphorylase inhibitors." Tetrahedron Letters 2006, 47, 6143-6147.
19. Peter G. Goekjian. "Staurosporine as an early lead: an overview of kinase inhibitors inspired by the indolocarbazole alkaloids." Dosis 2006, 22, 124-151.
20. David Gueyrard, Patrice Fontaine and Peter G. Goekjian. "Synthesis of C-glucoside endo-glycals from C-glucosyl vinyl sulfones." Synthesis 2006, 1499-1503.
21. Tahar Belhadj and Peter G. Goekjian. "An amide orthoesterification route to N -(1'-alkylthio-glucopyranosyl)indoles." Tetrahedron Letters 2005, 46, 8117-8120.
22. David Gueyrard, Rose Haddoub, Amine Salem, Nassib Said Bacar, and Peter G. Goekjian. "Synthesis of Exomethylene Glycals Using a Modified Julia Olefination." Synlett 2005 (3), 520-522.
23. Wendong Wang, Pornpun Rattananakin, and Peter G. Goekjian. "Synthesis of N-Glycoside Analogs via Thionolactones." J. Carb. Chem. 2003, 22, 743-751.
24. Peter G. Goekjian, Alexander Wei, and Yoshito Kishi. "Conformational Analysis of C-Glycosides and Related Compounds: Programming Conformational Profiles of C- and O-Glycosides" in Carbohydrate-based Drug Discovery, Wong, C.-H. Ed., Wiley 2003. Chapter 11, pp. 305-340.
25. Goekjian, P.G.; Jirousek, M. R. "Protein Kinase C Inhibitors as Novel Anticancer Drugs." Exp. Opin. Invest. Drugs 2001, 10, 2117-2140.
26. Wendong Wang, Guo-Zhang Wu, and Peter G. Goekjian. "Atypical Regioselectivity in the Electrochemical Reduction-Nucleophilic Substitution of Nitroanisole." Eur. J. Org. Chem., 2000, 1517-1520.
27. Peter G. Goekjian, Guo-Zhang Wu, Shi Chen, Lanxin Zhou, Michael R. Jirousek, James R. Gillig, Lawrence M. Ballas, and Jeffrey T. Dixon. "The Synthesis of Fluorinated Macrocyclic Bis(indolyl)maleimides as Potential 19F-NMR Probes for PKC." J. Org. Chem. 1999, 64, 4238-4246.
28. Peter G. Goekjian and Michael R. Jirousek. "Protein Kinase C in the Treatment of Disease: Signal transduction pathways, inhibitors, and agents in development." Current Med. Chem. 1999, 6, 877-903.
29. Michael R. Jirousek, Peter G. Goekjian, and Guo-Zhang Wu. "Halo-Substituted Protein Kinase C Inhibitors." United States patent number 5,936,084, August 10, 1999. Application pour le brevet international soumis le 1 Avril, 1997.
30. Peter G. Goekjian, Priscilla Lugo-Mas, Stacy L. Cable, John O. Cole, James W. White, Dale J. Thompson, Tamara P. Dudley, Michael R. Jirousek, Jeffrey T. Dixon, and Lawrence M. Ballas. "Synthesis of Indole-Ring Fluorine-Labeled Analogs of LY333531, an Isoform-Selective Inhibitor of PKC." J. Fluorine Chem. 1999, 98, 137-142.
31. W. Wang, G.-Z. Wu, and P. G. Goekjian. "Atypical Regioselectivity in the Electrochemical Reduction-Nucleophilic Substitution of Nitroanisole." Eur. J. Org. Chem., 2000, 1517-1520.
32. Edwin Vedejs, Rocco J. Galante, and Peter G. Goekjian. "A Thio-Diels-Alder Route to the Azocine Ring System. The Synthesis of (+/-)-Otonecine." J. Am. Chem. Soc. 1998, 120, 3613-3622.
33. Toru Haneda, Peter G. Goekjian, Sung H. Kim, and Yoshito Kishi. "Preferred Conformation of C-Glycosides. 10. Synthesis and Conformational Analysis of Carbon Trisaccharides" J. Org. Chem. 1992, 57, 490-498.
34. Yuan Wang, Peter G. Goekjian, David M. Ryckman, William H. Miller, Stefan A. Babirad, and Yoshito Kishi. "Preferred Conformation of C-Glycosides. 9. Conformational Analysis of 1,4-Linked Carbon Disaccharides" J. Org. Chem. 1992, 57, 482-489.
35. Peter G. Goekjian, Tse-Chong Wu, Han-Young Kang, and Yoshito Kishi. "Preferred Conformation of C-Glycosides. 7. Preferred Conformation of Carbon Analogues of Isomaltose and Gentiobiose." J. Org. Chem. 1991, 56, 6422-6434.
36. Peter G. Goekjian, Tse-Chong Wu, and Yoshito Kishi. "Preferred Conformation of C-Glycosides. 6. Conformational Similarity of Glycosides and Corresponding C-Glycosides." J. Org. Chem. 1991, 56, 6412-6422.
37. William H. Miller, David M. Ryckman, Peter G. Goekjian, Yuan Wang, and Yoshito Kishi. "Preferred Conformation of C-Glycosides. 5. Experimental Support for the Conformational Similarity between C- and O- Disaccharides." J. Org. Chem. 1988, 53, 5580-5582.
38. Yuan Wang, Peter G. Goekjian, David M. Ryckman, and Yoshito Kishi. "Preferred Confor-mation of C-Glycosides. 4. Importance of 1,3-Diaxial-like Interactions Around the Non-Glycosidic Bond: Prediction and Experimental Proof." J. Org. Chem. 1988, 53, 4151-4153.
39. Stefan A. Babirad, Yuan Wang, Peter G. Goekjian, and Yoshito Kishi. "Preferred Conformation of C-Glycosides. 3. Preferred Conformation of Carbon Analogues of 1,4-Disaccharides." J. Org. Chem. 1987, 52, 4825-4827.
40. Peter G. Goekjian, Tse-Chong Wu, Han-Young Kang, and Yoshito Kishi. "Preferred Conformation of C-Glycosides. 2. Preferred Conformation of Carbon Analogues of Isomaltose and Gentiobiose." J. Org. Chem. 1987, 52, 4823-4825.
41. Tse-Chong Wu, Peter G. Goekjian, and Yoshito Kishi. "Preferred Conformation of C-Glycosides. 1. Conformational Similarity of Glycosides and Corresponding C-Glycosides." J. Org. Chem. 1987, 52, 4819-4823.