 5 Beechmount building, 34 old bakers court, BT6 8QY, Belfast
                         United Kingdom                                            Nicolas
                      0044 7 837 567 783
                E-mail: Nicolas.wlod@gmail.com                                 Wlodarczyk, PhD
                                                                               Dynamic, open-minded, diligent




                                            HIGHLIGHTS
     Strong knowledge and experience in synthetic organic and medicinal chemistry
     Design of small bioactive and lead optimization for pre-clinical candidate
     Supervisor of many internship students for 1 to 9 months
     Key contributor in interdisciplinary research projects
     6 publications in peer reviewed journal and numerous presentations (posters and seminars)

                                                 SKILLS
     Synthesis: Heterocyclic chemistry, multi-step synthesis, solid phase synthesis (parallel synthesis),
      microwave synthesis, flow chemistry
     Analytical techniques: NMR, HPLC, GC, IR, UV, LC-MS, DLS
     Special skills: cheminformatic (Discovery Studio)
     Bibliographic seeking: Scifinder, Reaxys, RSS feed
     Computer skills: Word, Excel, Power Point, ISIS Draw, Chemdraw, ISIS Base, Photoshop, E-
      notebook, Chembridge molecular library
     Languages: English (expert), French (native)


                                             EDUCATION
PhD in Synthetic organic and medicinal chemistry with an excellent mention                             2008
Lille 2 University - France
MD in Drug Design with an excellent mention                                                            2005
Lille 2 University - France
BSc in Pharmaceutical sciences with an excellent mention                                               2003
Lille 2 University – France
Diploma of technician                                                                                  2002
Lille 1 University – France
French baccalaureate specialized in chemistry with an excellent mention                                2000
Valentine Labbé High school, La Madeleine - France

                                           EXPERIENCES
                               Medicinal Chemist (from February 2012)
     ALMAC Discovery (Research and Development department), Craigavon, Northern Ireland
     Subjects: Different confidential patented subjects which change in function of the results and the
      deadlines
     Hit finding: resynthesis and study of the stability (LCMS and NMR) to validate the hits, then establish
      some SAR to prepare some series which are chosen in function of the patentability and the
      preliminary biological results
   Lead optimization: chemical modification of potent compounds to improve ADME parameter
    (solubility, stability, pharmacokinetic, toxicity), to select any of those to preclinical studies

              Temporary research associate (September 2011 to October 2009)
   Laboratory of Medicinal Chemistry, URA(CNRS)2128, Institut Pasteur, Paris, France
   Supervisor: Y.L. Janin, PhD
   Research subject: Design, synthesis of parasitic serine protease inhibitors (confidential)
   Optimization of the synthesis of the chemical scaffolds (quinoline) to prepare chemical libraries
   Interdisciplinary exchange between chemistry, biology (in vitro and in vivo activity), biophysic (STD-
    NMR, X-Ray crystallography) and bioinformatic (docking and QSAR)
   Measurement of small molecules aggregation by Dynamic Light Scattering (DLS)
   Results: 1 publication (other publications and patents are in preparation), 200 compounds prepared
    on different series, detection of nuisance compounds

                       Temporary lecturer (August 2009 to October 2008)
   Laboratory of Pharmacological and Toxicological Chemistry and Biochemistry, UMR(CNRS)8601,
    Paris Descartes University, France
   Supervisor: Y. Le Merrer, Pr., team leader
   Courses teaching: organic and inorganic chemistry in license degree
   Research subject: Design, synthesis and biological evaluation of methionine aminopeptidase
    inhibitors in cancer treatment

                           PhD internship (September 2008 to September 2005)
   Faculty of Pharmacy, Lille II University, France
   Supervisor: J-P. Hénichart, Pr., team leader
   Research subject: Design, synthesis and pharmacological evaluation of farnesyltransferase
    inhibitors in cancer treatment
   Heterocyclic chemistry (1,4-diazepane and 4-aminopiperidine) and Parallel synthesis on solid phase
   Assay by myself of my inhibitors by enzymatic assay (fluorescence method)
   Rationalization of in vitro and in vivo results from docking studies and physical parameters
   Results: 5 publications, structure-activity relationships to design a promising pharmcophore, good in
    vitro and in vivo inhibitors

                        Internship as technician (July 2005 to October 2002)
   Faculty of Pharmacy, Lille II University, France
   Supervisor: J-P. Hénichart, Pr., team leader
   Acquired essential laboratory skills by: synthesizing heterocyclic compounds, purifying by usual
    techniques as extraction, recrystallization, flash chromatography and analyzing by chromatography
    (TLC, HPLC, LCMS) and spectroscopic methods (IR, NMR and MS)
   Supervised many students during their trainee period (1 week to 9 months)
   Synthesis of heterocyclic compounds for Genfit (CRO, LOOS, France), patent WO2008/012470




                                        PUBLICATIONS
1. On the Knorr synthesis of 6-bromo-4-methylquinolin-2(1H)-one. Wlodarczyk N., Simenel C.,
   Delepierre M., Barale J-C. Janin Y. L. Synthesis, 2011, 6, 934-942
2. Potent farnesyltransferase inhibitors with 1,4-diazepane scaffolds as novel destabilizing microtubule
   agents in hormone-resistant prostate cancer. Wlodarczyk N., Ryckewaert D., Gilleron P., Lemoine
   A., Farce A., Chavatte P., Dubois J., Pommery N., J-P. Hénichart, Millet R. J. Med. Chem., 2011, 54,
   1178-1190

3. Design, synthesis and biological evaluation of substituted dioxodibenzothiazepines and
   dibenzocycloheptanes as farnesyltransferase inhibitors. Gilleron P., Wlodarczyk N., Houssin R.,
   Farce A., Laconde G., Goossens J-F., Lemoine A., Pommery N., Hénichart J-P., Millet R. Bioorg.
   Med. Chem. Lett., 2007, 17, 5465-5471

4. Synthesis of 1,4-diazepin-5-ones under microwave irradiation and their reduction products
   Wlodarczyk N., Gilleron P., Millet R., Houssin R., Hénichart J.-P. Tetrahedron Lett., 2007, 48, 2583-
   2586

5. Solid-phase synthesis and pharmacological evaluation of a library of peptidomimetics as potential
   farnesyltransferase inhibitors: an approach to new lead compounds. Gilleron P., Millet R., Houssin R.,
   Wlodarczyk N., Farce A., Lemoine A., Goossens J-F., Chavatte P., Pommery N., Henichart J-P. Eur.
   J. Med. Chem., 2006, 41,745-55

6. In vitro and in vivo evaluation of two rational-designed nonpeptidic farnesyltransferase inhibitors on
   HT29 human colon cancer cell lines. Wlodarczyk N., Gilleron P., Millet R., Houssin R., Goossens J.-
   F., Lemoine A., Pommery N., Wei M. X., Hénichart J.-P. Oncol. Res., 2005, 16, 107-118

   PUBLISHED ABSTRACTS AND CONFERENCE PRESENTATIONS
                                         (only the most important)
Design, synthesis of novel farnesyltransferase inhibitors as novel microtubule-destabilizing agents in PC3
cells. N. Wlodarczyk, D. Ryckewaert, P. Gilleron, A. Lemoine, A Farce, C. Furman, J. Dubois, P.
Chavatte, J-P. Henichart, R. Millet. 21st International Symposium of Medicinal Chemistry, Brussel
(Belgium), September 5-9 2010

Design, synthesis and pharmacological evaluation of potent farnesyltransferase inhibitors with the 1,4-
diazepane scaffold. N. Wlodarczyk, P. Gilleron, P. Six, A. Lemoine, A Farce, R. Houssin, P. Chavatte, J.
                                     st
Dubois, J-P. Henichart, R. Millet. 44 International Meeting of Therapeutic Chemistry, Angers (France),
Jully 1-4 2008
Award for the Vocation in Therapeutic Chemistry (from Servier)

Design, synthesis and pharmacological evaluation of potent farnesyltransferase inhibitors with 7-phenyl-
1,4-diazepane scaffold. Wlodarczyk N., Gilleron P., Lemoine A., Dubois J., Pommery N., Houssin R.,
                            th
Hénichart J-P., Millet R. 15 Young Researchers Day of the French Society of Therapeutic Chemistry
                            st
(France), Paris, January 31 2008

Cv

  • 1.
     5 Beechmountbuilding, 34 old bakers court, BT6 8QY, Belfast United Kingdom Nicolas  0044 7 837 567 783 E-mail: Nicolas.wlod@gmail.com Wlodarczyk, PhD Dynamic, open-minded, diligent HIGHLIGHTS  Strong knowledge and experience in synthetic organic and medicinal chemistry  Design of small bioactive and lead optimization for pre-clinical candidate  Supervisor of many internship students for 1 to 9 months  Key contributor in interdisciplinary research projects  6 publications in peer reviewed journal and numerous presentations (posters and seminars) SKILLS  Synthesis: Heterocyclic chemistry, multi-step synthesis, solid phase synthesis (parallel synthesis), microwave synthesis, flow chemistry  Analytical techniques: NMR, HPLC, GC, IR, UV, LC-MS, DLS  Special skills: cheminformatic (Discovery Studio)  Bibliographic seeking: Scifinder, Reaxys, RSS feed  Computer skills: Word, Excel, Power Point, ISIS Draw, Chemdraw, ISIS Base, Photoshop, E- notebook, Chembridge molecular library  Languages: English (expert), French (native) EDUCATION PhD in Synthetic organic and medicinal chemistry with an excellent mention 2008 Lille 2 University - France MD in Drug Design with an excellent mention 2005 Lille 2 University - France BSc in Pharmaceutical sciences with an excellent mention 2003 Lille 2 University – France Diploma of technician 2002 Lille 1 University – France French baccalaureate specialized in chemistry with an excellent mention 2000 Valentine Labbé High school, La Madeleine - France EXPERIENCES Medicinal Chemist (from February 2012)  ALMAC Discovery (Research and Development department), Craigavon, Northern Ireland  Subjects: Different confidential patented subjects which change in function of the results and the deadlines  Hit finding: resynthesis and study of the stability (LCMS and NMR) to validate the hits, then establish some SAR to prepare some series which are chosen in function of the patentability and the preliminary biological results
  • 2.
    Lead optimization: chemical modification of potent compounds to improve ADME parameter (solubility, stability, pharmacokinetic, toxicity), to select any of those to preclinical studies Temporary research associate (September 2011 to October 2009)  Laboratory of Medicinal Chemistry, URA(CNRS)2128, Institut Pasteur, Paris, France  Supervisor: Y.L. Janin, PhD  Research subject: Design, synthesis of parasitic serine protease inhibitors (confidential)  Optimization of the synthesis of the chemical scaffolds (quinoline) to prepare chemical libraries  Interdisciplinary exchange between chemistry, biology (in vitro and in vivo activity), biophysic (STD- NMR, X-Ray crystallography) and bioinformatic (docking and QSAR)  Measurement of small molecules aggregation by Dynamic Light Scattering (DLS)  Results: 1 publication (other publications and patents are in preparation), 200 compounds prepared on different series, detection of nuisance compounds Temporary lecturer (August 2009 to October 2008)  Laboratory of Pharmacological and Toxicological Chemistry and Biochemistry, UMR(CNRS)8601, Paris Descartes University, France  Supervisor: Y. Le Merrer, Pr., team leader  Courses teaching: organic and inorganic chemistry in license degree  Research subject: Design, synthesis and biological evaluation of methionine aminopeptidase inhibitors in cancer treatment PhD internship (September 2008 to September 2005)  Faculty of Pharmacy, Lille II University, France  Supervisor: J-P. Hénichart, Pr., team leader  Research subject: Design, synthesis and pharmacological evaluation of farnesyltransferase inhibitors in cancer treatment  Heterocyclic chemistry (1,4-diazepane and 4-aminopiperidine) and Parallel synthesis on solid phase  Assay by myself of my inhibitors by enzymatic assay (fluorescence method)  Rationalization of in vitro and in vivo results from docking studies and physical parameters  Results: 5 publications, structure-activity relationships to design a promising pharmcophore, good in vitro and in vivo inhibitors Internship as technician (July 2005 to October 2002)  Faculty of Pharmacy, Lille II University, France  Supervisor: J-P. Hénichart, Pr., team leader  Acquired essential laboratory skills by: synthesizing heterocyclic compounds, purifying by usual techniques as extraction, recrystallization, flash chromatography and analyzing by chromatography (TLC, HPLC, LCMS) and spectroscopic methods (IR, NMR and MS)  Supervised many students during their trainee period (1 week to 9 months)  Synthesis of heterocyclic compounds for Genfit (CRO, LOOS, France), patent WO2008/012470 PUBLICATIONS 1. On the Knorr synthesis of 6-bromo-4-methylquinolin-2(1H)-one. Wlodarczyk N., Simenel C., Delepierre M., Barale J-C. Janin Y. L. Synthesis, 2011, 6, 934-942
  • 3.
    2. Potent farnesyltransferaseinhibitors with 1,4-diazepane scaffolds as novel destabilizing microtubule agents in hormone-resistant prostate cancer. Wlodarczyk N., Ryckewaert D., Gilleron P., Lemoine A., Farce A., Chavatte P., Dubois J., Pommery N., J-P. Hénichart, Millet R. J. Med. Chem., 2011, 54, 1178-1190 3. Design, synthesis and biological evaluation of substituted dioxodibenzothiazepines and dibenzocycloheptanes as farnesyltransferase inhibitors. Gilleron P., Wlodarczyk N., Houssin R., Farce A., Laconde G., Goossens J-F., Lemoine A., Pommery N., Hénichart J-P., Millet R. Bioorg. Med. Chem. Lett., 2007, 17, 5465-5471 4. Synthesis of 1,4-diazepin-5-ones under microwave irradiation and their reduction products Wlodarczyk N., Gilleron P., Millet R., Houssin R., Hénichart J.-P. Tetrahedron Lett., 2007, 48, 2583- 2586 5. Solid-phase synthesis and pharmacological evaluation of a library of peptidomimetics as potential farnesyltransferase inhibitors: an approach to new lead compounds. Gilleron P., Millet R., Houssin R., Wlodarczyk N., Farce A., Lemoine A., Goossens J-F., Chavatte P., Pommery N., Henichart J-P. Eur. J. Med. Chem., 2006, 41,745-55 6. In vitro and in vivo evaluation of two rational-designed nonpeptidic farnesyltransferase inhibitors on HT29 human colon cancer cell lines. Wlodarczyk N., Gilleron P., Millet R., Houssin R., Goossens J.- F., Lemoine A., Pommery N., Wei M. X., Hénichart J.-P. Oncol. Res., 2005, 16, 107-118 PUBLISHED ABSTRACTS AND CONFERENCE PRESENTATIONS (only the most important) Design, synthesis of novel farnesyltransferase inhibitors as novel microtubule-destabilizing agents in PC3 cells. N. Wlodarczyk, D. Ryckewaert, P. Gilleron, A. Lemoine, A Farce, C. Furman, J. Dubois, P. Chavatte, J-P. Henichart, R. Millet. 21st International Symposium of Medicinal Chemistry, Brussel (Belgium), September 5-9 2010 Design, synthesis and pharmacological evaluation of potent farnesyltransferase inhibitors with the 1,4- diazepane scaffold. N. Wlodarczyk, P. Gilleron, P. Six, A. Lemoine, A Farce, R. Houssin, P. Chavatte, J. st Dubois, J-P. Henichart, R. Millet. 44 International Meeting of Therapeutic Chemistry, Angers (France), Jully 1-4 2008 Award for the Vocation in Therapeutic Chemistry (from Servier) Design, synthesis and pharmacological evaluation of potent farnesyltransferase inhibitors with 7-phenyl- 1,4-diazepane scaffold. Wlodarczyk N., Gilleron P., Lemoine A., Dubois J., Pommery N., Houssin R., th Hénichart J-P., Millet R. 15 Young Researchers Day of the French Society of Therapeutic Chemistry st (France), Paris, January 31 2008