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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).
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, France.
EA 4421 SiGReTO, Université de Lorraine, Faculté de pharmacie, 5-7 Rue Albert Lebrun, BP80403, 54001 Nancy cedex, France.
Rome 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.
Rome 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.ORCID iD: 0000-0002-4831-3423
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2013 (English)In: European Journal of Medicinal Chemistry, ISSN 0223-5234, E-ISSN 1768-3254, Vol. 63, 765-81 p., S0223-5234(13)00170-0Article in journal (Refereed) Published
Abstract [en]

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.

Place, publisher, year, edition, pages
Elsevier, 2013. Vol. 63, 765-81 p., S0223-5234(13)00170-0
Keyword [en]
Vascular endothelial growth factor receptor-2 (VEGFR-2), Anti-angiogenic activity, Structure-based drug design (SBDD), Ligand-based drug design (LBDD), 3D QSAR, Thieno[3, 2-d]pyrimidinone, Thieno[1, 2, 3]triazine, Endothelial cell tube formation
National Category
Medicinal Chemistry Chemical Sciences Biological Sciences Computer and Information Science
Identifiers
URN: urn:nbn:se:uu:diva-321305DOI: 10.1016/j.ejmech.2013.03.022PubMedID: 23583911OAI: oai:DiVA.org:uu-321305DiVA: diva2:1094955
Available from: 2017-05-11 Created: 2017-05-11 Last updated: 2017-05-12

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