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  • Perspicace, EnricoLaboratoire d ’ Ingénierie Moléculaire et Biochimie Pharmacologique, UMR CNRS 7565 SRSMC, Institut Jean Barriol, FR CNRS 2843, Université de Lorraine, 1 Boulevard Arago, 57070 Metz, France (author)

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).

  • Article/chapterEnglish2013

Publisher, publication year, extent ...

  • Elsevier,2013
  • printrdacarrier

Numbers

  • LIBRIS-ID:oai:DiVA.org:uu-321305
  • https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-321305URI
  • https://doi.org/10.1016/j.ejmech.2013.03.022DOI

Supplementary language notes

  • Language:English
  • Summary in:English

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  • Subject category:ref swepub-contenttype
  • Subject category:art swepub-publicationtype

Notes

  • Driven by a multidisciplinary approach combination (Structure-Based (SB) Three-Dimensional Quantitative Structure-Activity Relationships (3-D QSAR), molecular modeling, organic chemistry and various biological evaluations) here is reported the disclosure of new thienopyrimidines 1-3 as inhibitors of KDR activity and human umbilical vein endothelial cell (HUVEC) proliferation. More specifically, compound 2f represents a new lead compound that inhibits VEGFR-2 and HUVEC at μM concentration. Moreover by the mean of an endothelial cell tube formation in vitro model 2f tartaric acid salt proved to block angiogenesis of HUVEC at μM level.

Subject headings and genre

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  • Jouan-Hureaux, ValérieEA 4421 SiGReTO, Université de Lorraine, Faculté de pharmacie, 5-7 Rue Albert Lebrun, BP80403, 54001 Nancy cedex, France (author)
  • Ragno, RinoRome Center for Molecular Design, Dipartimento di Chimica e Tecnologie del Farmaco, Università degli Studi di Roma “ La Sapienza ” , P. le A. Moro 5, 00185 Roma, Italy (author)
  • Ballante, FlavioRome Center for Molecular Design, Dipartimento di Chimica e Tecnologie del Farmaco, Università degli Studi di Roma “ La Sapienza ” , P. le A. Moro 5, 00185 Roma, Italy(Swepub:uu)flaba767 (author)
  • Sartini, StefaniaDipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy (author)
  • La Motta, ConcettinaDipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy (author)
  • Da Settimo, FedericoDipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy (author)
  • Chen, BinbinLaboratoire d ’ Ingénierie Moléculaire et Biochimie Pharmacologique, UMR CNRS 7565 SRSMC, Institut Jean Barriol, FR CNRS 2843, Université de Lorraine, 1 Boulevard Arago, 57070 Metz, France (author)
  • Kirsch, GilbertLaboratoire d ’ Ingénierie Moléculaire et Biochimie Pharmacologique, UMR CNRS 7565 SRSMC, Institut Jean Barriol, FR CNRS 2843, Université de Lorraine, 1 Boulevard Arago, 57070 Metz, France (author)
  • Schneider, SergeLaboratoire National de Santé, Division de Toxicologie, Université de Luxembourg, 162a Avenue de la Faïencerie, L-1511 Luxembourg, Luxembourg (author)
  • Faivre, BéatriceEA 4421 SiGReTO, Université de Lorraine, Faculté de pharmacie, 5-7 Rue Albert Lebrun, BP80403, 54001 Nancy cedex, France (author)
  • Hesse, StéphanieLaboratoire d ’ Ingénierie Moléculaire et Biochimie Pharmacologique, UMR CNRS 7565 SRSMC, Institut Jean Barriol, FR CNRS 2843, Université de Lorraine, 1 Boulevard Arago, 57070 Metz, France (author)
  • Laboratoire d ’ Ingénierie Moléculaire et Biochimie Pharmacologique, UMR CNRS 7565 SRSMC, Institut Jean Barriol, FR CNRS 2843, Université de Lorraine, 1 Boulevard Arago, 57070 Metz, FranceEA 4421 SiGReTO, Université de Lorraine, Faculté de pharmacie, 5-7 Rue Albert Lebrun, BP80403, 54001 Nancy cedex, France (creator_code:org_t)

Related titles

  • In:European Journal of Medicinal Chemistry: Elsevier63, s. 765-810223-52341768-3254

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