Papadopoulou Lefkothea
Concettina La Motta, PhD
Associate Professor of Medicinal Chemistry
  • University of Pisa
    Pisa, Italy
    E-mail: concettina.lamotta@unipi.it
    Phone: +30 050 2219593

     

Education

 

Biography

Concettina La Motta graduated cum laude in the long-term degree course of Pharmaceutical Chemistry and Technology, in 1992, at the Faculty of Pharmacy of the University of Pisa, Italy. From 1992 to 1996 she worked at the pharmaceutical company Farmigea S.p.A, Research and Development Division, than she obtained her PhD in Medicinal Chemistry, in 1999. Assistant Professor, from 2000 to 2011, she now works as associate professor of medicinal chemistry at the Department of Pharmacy of the University of Pisa, Italy.
She is the author of more than 140 publications in the fields of medicinal chemistry, including research articles in leading international journals, national and international patents, chapters in books, published by major presses, and a number of oral and poster communications at national and international congresses. On the basis of her researches, many students have been awarded their master and Ph.D degrees in medicinal chemistry.

She serves as reviewer of papers for publishers like the American Chemical Society Publication, Elsevier Ltd, Wiley Interscience, and RSC Journals, as well as reviewer of research proposals for agencies like the Italian and European Ministries of Education and Research.

Research Interest

  • Design and the synthesis of novel inhibitors of enzymes like tyrosine kinases, ALR2,COX2, and ADA
  • To develop as drug candidates for the treatment of inflammation and cancer

 

 

Professional Activities:

Teaching Experience(undergraduate and master's degree):

Positions of responsibility of teaching modules/lessons

  • Teaching of Food Chemistry (Cod. 242CC) for Single Cycle Degree five years in Chemistry and Pharmaceutical Technology.
  • Teaching of Food Chemistry (Cod. 267CC) for the degree course in Sciences Human Nutrition.
  • Teaching of Pharmaceutical Biotechnology (Cod. 255CC) for Single Cycle Degree five years in Chemistry and Pharmaceutical Technology.
  • Teachings shared / borrowed:
Pharmaceutical Biotechnology (Cod. 249CC) - Single Cycle Degree in Pharmacy 5 years
Positions of co-teaching in modules / lessons

Teaching of Pharmaceutical Chemistry and Toxicology II (Cod. 028CC) for Single Cycle Degree five years in Chemistry and Pharmaceutical Technology.

Publications

  1. Salerno S, Marini AM, Fornaciari G, Simorini F, La Motta C, Taliani S, Sartini S, Da Settimo F, García-Argáez AN, Gia O, Cosconati S, Novellino E, D'Ocon P, Fioravanti A, Orlandi P, Bocci G, Dalla Via L. Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2. Eur J Med Chem. 2015 Oct 20;103:29-43. doi: 10.1016/j.ejmech.2015.08.027.
  2. Fallahi P, Ferrari SM, La Motta C, Materazzi G, Bocci G, Da Settimo F, Miccoli P, Antonelli A. CLM29 and CLM24, pyrazolopyrimidine derivatives, have antitumoral activity in vitro in anaplastic thyroid cancer, with or without BRAF mutation. Endocrine. 2015 Aug 19.
  3. Barresi E, Bruno A, Taliani S, Cosconati S, Da Pozzo E, Salerno S, Simorini F, Daniele S, Giacomelli C, Marini AM, La Motta C, Marinelli L, Cosimelli B, Novellino E, Greco G, Da Settimo F, Martini C. Deepening the Topology of the Translocator Protein Binding Site by Novel N,N-Dialkyl-2-arylindol-3-ylglyoxylamides. J Med Chem. 2015 Aug 13;58(15):6081-92. doi: 10.1021/acs.jmedchem.5b00689.
  4. Consalvi S, Alfonso S, Di Capua A, Poce G, Pirolli A, Sabatino M, Ragno R, Anzini M, Sartini S, La Motta C, Di Cesare Mannelli L, Ghelardini C, Biava M. Synthesis, biological evaluation and docking analysis of a new series of methylsulfonyl and sulfamoyl acetamides and ethyl acetates as potent COX-2 inhibitors. Bioorg Med Chem. 2015 Feb 15;23(4):810-20. doi: 10.1016/j.bmc.2014.12.041.
  5. Del Turco S, Sartini S, Cigni G, Sentieri C, Sbrana S, Battaglia D, Papa A, Da Settimo F, La Motta C, Basta G. Synthetic analogues of flavonoids with improved activity against platelet activation and aggregation as novel prototypes of food supplements. Food Chem. 2015 May 15;175:494-9. doi: 10.1016/j.foodchem.2014.12.005.
  6. Di Filippo C, Zippo MV, Maisto R, Trotta MC, Siniscalco D, Ferraro B, Ferraraccio F, La Motta C, Sartini S, Cosconati S, Novellino E, Gesualdo C, Simonelli F, Rossi S, D'Amico M. Inhibition of ocular aldose reductase by a new benzofuroxane derivative ameliorates rat endotoxic uveitis. Mediators Inflamm. 2014;2014:857958. doi: 10.1155/2014/857958.
  7. Ferrari SM, Fallahi P, La Motta C, Bocci G, Corrado A, Materazzi G, Galleri D, Piaggi S, Danesi R, Da Settimo F, Miccoli P, Antonelli A. Antineoplastic activity of the multitarget tyrosine kinase inhibitors CLM3 and CLM94 in medullary thyroid cancer in vitro. Surgery. 2014 Nov;156(5):1167-76. doi: 10.1016/j.surg.2014.05.005.
  8. Antonelli A, Bocci G, La Motta C, Ferrari SM, Fallahi P, Corrado A, Fioravanti A, Sartini S, Orlandi P, Piaggi S, Corti A, Materazzi G, Galleri D, Ulisse S, Fontanini G, Danesi R, Da Settimo F, Miccoli P. CLM29, a multi-target pyrazolopyrimidine derivative, has anti-neoplastic activity in medullary thyroid cancer in vitro and in vivo. Mol Cell Endocrinol. 2014 Aug 5;393(1-2):56-64. doi: 10.1016/j.mce.2014.06.002.
  9. Sartini S, Coviello V, Bruno A, La Pietra V, Marinelli L, Simorini F, Taliani S, Salerno S, Marini AM, Fioravanti A, Orlandi P, Antonelli A, Da Settimo F, Novellino E, Bocci G, La Motta C. Structure-based optimization of tyrosine kinase inhibitor CLM3. Design, synthesis, functional evaluation, and molecular modeling studies. J Med Chem. 2014 Feb 27;57(4):1225-35. doi: 10.1021/jm401358b.
  10. Antonelli A, Bocci G, Fallahi P, La Motta C, Ferrari SM, Mancusi C, Fioravanti A, Di Desidero T, Sartini S, Corti A, Piaggi S, Materazzi G, Spinelli C, Fontanini G, Danesi R, Da Settimo F, Miccoli P. CLM3, a multitarget tyrosine kinase inhibitor with antiangiogenic properties, is active against primary anaplastic thyroid cancer in vitro and in vivo. J Clin Endocrinol Metab. 2014 Apr;99(4):E572-81. doi: 10.1210/jc.2013-2321.
  11. Del Turco S, Sartini S, Sentieri C, Saponaro C, Navarra T, Dario B, Da Settimo F, La Motta C, Basta G. A novel 2,3-diphenyl-4H-pyrido[1,2-a]pyrimidin-4-one derivative inhibits endothelial cell dysfunction and smooth muscle cell proliferation/activation. Eur J Med Chem. 2014 Jan 24;72:102-9. doi: 10.1016/j.ejmech.2013.11.021.
  12. Redolfi Riva E, Desii A, Sartini S, La Motta C, Mazzolai B, Mattoli V. PMMA/polysaccharides nanofilm loaded with adenosine deaminase inhibitor for targeted anti-inflammatory drug delivery. Langmuir. 2013 Oct 29;29(43):13190-7. doi: 10.1021/la402229k.
  13. Del-Corso A, Balestri F, Di Bugno E, Moschini R, Cappiello M, Sartini S, La-Motta C, Da-Settimo F, Mura U. A new approach to control the enigmatic activity of aldose reductase. PLoS One. 2013 Sep 3;8(9):e74076. doi: 10.1371/journal.pone.0074076.
  14. Taliani S, Pugliesi I, Barresi E, Salerno S, Marchand C, Agama K, Simorini F, La Motta C, Marini AM, Di Leva FS, Marinelli L, Cosconati S, Novellino E, Pommier Y, Di Santo R, Da Settimo F. Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors. J Med Chem. 2013 Sep 26;56(18):7458-62. doi: 10.1021/jm400932c.
  15. Perspicace E, Jouan-Hureaux V, Ragno R, Ballante F, Sartini S, La Motta C, Da Settimo F, Chen B, Kirsch G, Schneider S, Faivre B, Hesse S. Design, synthesis and biological evaluation of new classes of thieno[3,2-d]pyrimidinone and thieno[1,2,3]triazine as inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2). Eur J Med Chem. 2013 May;63:765-81. doi: 10.1016/j.ejmech.2013.03.022.
  16. Sartini S, Cosconati S, Marinelli L, Barresi E, Di Maro S, Simorini F, Taliani S, Salerno S, Marini AM, Da Settimo F, Novellino E, La Motta C. Benzofuroxane derivatives as multi-effective agents for the treatment of cardiovascular diabetic complications. Synthesis, functional evaluation, and molecular modeling studies. J Med Chem. 2012 Dec 13;55(23):10523-31. doi: 10.1021/jm301124s.
  17. Marini AM, Maresca A, Aggarwal M, Orlandini E, Nencetti S, Da Settimo F, Salerno S, Simorini F, La Motta C, Taliani S, Nuti E, Scozzafava A, McKenna R, Rossello A, Supuran CT. Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms. J Med Chem. 2012 Nov 26;55(22):9619-29. doi: 10.1021/jm300878g.
  18. Ramunno A, Cosconati S, Sartini S, Maglio V, Angiuoli S, La Pietra V, Di Maro S, Giustiniano M, La Motta C, Da Settimo F, Marinelli L, Novellino E. Progresses in the pursuit of aldose reductase inhibitors: the structure-based lead optimization step. Eur J Med Chem. 2012 May;51:216-26. doi: 10.1016/j.ejmech.2012.02.045.
  19. Antonelli A, Bocci G, La Motta C, Ferrari SM, Fallahi P, Ruffilli I, Di Domenicantonio A, Fioravanti A, Sartini S, Minuto M, Piaggi S, Corti A, Alì G, Di Desidero T, Berti P, Fontanini G, Danesi R, Da Settimo F, Miccoli P. CLM94, a novel cyclic amide with anti-VEGFR-2 and antiangiogenic properties, is active against primary anaplastic thyroid cancer in vitro and in vivo. J Clin Endocrinol Metab. 2012 Apr;97(4):E528-36. doi: 10.1210/jc.2011-1987.
  20. Taliani S, Pugliesi I, Barresi E, Simorini F, Salerno S, La Motta C, Marini AM, Cosimelli B, Cosconati S, Di Maro S, Marinelli L, Daniele S, Trincavelli ML, Greco G, Novellino E, Martini C, Da Settimo F. 3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A₂B adenosine receptor antagonists. J Med Chem. 2012 Feb 23;55(4):1490-9. doi: 10.1021/jm201177b.
  21. Antonioli L, Colucci R, La Motta C, Tuccori M, Awwad O, Da Settimo F, Blandizzi C, Fornai M. Adenosine deaminase in the modulation of immune system and its potential as a novel target for treatment of inflammatory disorders. Curr Drug Targets. 2012 Jun;13(6):842-62. Review.
  22. Limongelli V, Marinelli L, Cosconati S, La Motta C, Sartini S, Mugnaini L, Da Settimo F, Novellino E, Parrinello M. Sampling protein motion and solvent effect during ligand binding. Proc Natl Acad Sci U S A. 2012 Jan 31;109(5):1467-72. doi: 10.1073/pnas.1112181108.
  23. Sartini S, Morelli M, Simorini F, Taliani S, Salerno S, Marini AM, Da Settimo F, La Motta C. Geometrically constrained derivatives of indolylglyoxylamides as ligands binding the GABAA/BzR complex. Curr Top Med Chem. 2012;12(4):312-20. Review.
  24. Simorini F, Marini AM, Taliani S, La Motta C, Salerno S, Pugliesi I, Da Settimo F. Medicinal chemistry of indolylglyoxylamide TSPO high affinity ligands with anxiolytic-like effects. Curr Top Med Chem. 2012;12(4):333-51. Review.
  25. Salerno S, Da Settimo F, Taliani S, Simorini F, La Motta C, Fornaciari G, Marini AM. Medicinal chemistry of indolylglyoxylamide GABAA/BzR high affinity ligands: identification of novel anxiolytic/non sedative agents. Curr Top Med Chem. 2012;12(4):286-311. Review.
  26. La Pietra V, Marinelli L, Cosconati S, Di Leva FS, Nuti E, Santamaria S, Pugliesi I, Morelli M, Casalini F, Rossello A, La Motta C, Taliani S, Visse R, Nagase H, da Settimo F, Novellino E. Identification of novel molecular scaffolds for the design of MMP-13 inhibitors: a first round of lead optimization. Eur J Med Chem. 2012 Jan;47(1):143-52. doi: 10.1016/j.ejmech.2011.10.035.
  27. Cosimelli B, Simorini F, Taliani S, La Motta C, Da Settimo F, Severi E, Greco G, Novellino E, Costa B, Da Pozzo E, Bendinelli S, Martini C. Tertiary amides with a five-membered heteroaromatic ring as new probes for the translocator protein. Eur J Med Chem. 2011 Sep;46(9):4506-20. doi: 10.1016/j.ejmech.2011.07.025.
  28. Cosimelli B, Taliani S, Greco G, Novellino E, Sala A, Severi E, Da Settimo F, La Motta C, Pugliesi I, Antonioli L, Fornai M, Colucci R, Blandizzi C, Daniele S, Trincavelli ML, Martini C. Derivatives of benzimidazol-2-ylquinoline and benzimidazol-2-ylisoquinoline as selective A1 adenosine receptor antagonists with stimulant activity on human colon motility. ChemMedChem. 2011 Oct 4;6(10):1909-18. doi: 10.1002/cmdc.201100284.
  29. Sartini S, Dario B, Morelli M, Da Settimo F, La Motta C. Receptor tyrosine kinase kit and gastrointestinal stromal tumours: an overview. Curr Med Chem. 2011;18(19):2893-903. Review.
  30. Ottanà R, Maccari R, Giglio M, Del Corso A, Cappiello M, Mura U, Cosconati S, Marinelli L, Novellino E, Sartini S, La Motta C, Da Settimo F.

 

 

Durg-research-flyer