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 …

E Perspicace, V Jouan-Hureaux, R Ragno…

Index: Perspicace, Enrico; Jouan-Hureaux, Valerie; Ragno, Rino; Ballante, Flavio; Sartini, Stefania; La Motta, Concettina; Da Settimo, Federico; Chen, Binbin; Kirsch, Gilbert; Schneider, Serge; Faivre, Beatrice; Hesse, Stephanie European Journal of Medicinal Chemistry, 2013 , vol. 63, p. 765 - 781

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Citation Number: 24

Abstract

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 ...