51721-68-7Relevant articles and documents
Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity
Luo, Guoshun,Tang, Zhichao,Lao, Kejing,Li, Xinyu,You, Qidong,Xiang, Hua
, p. 783 - 795 (2018/04/02)
Both ERα and VEGFR-2 are important targets for cancer therapies. Here a series of 2, 4-disubstituted pyrimidine derivatives were designed, synthesized and evaluated as dual ERα/VEGFR-2 ligands. Most of the derivatives exhibited potent activities in both e
Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d[pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2
Salerno, Silvia,Marini, Anna Maria,Fornaciari, Giacomo,Simorini, Francesca,La Motta, Concettina,Taliani, Sabrina,Sartini, Stefania,Da Settimo, Federico,Garciá-Argaéz, Aída Nelly,Gia, Ornella,Cosconati, Sandro,Novellino, Ettore,D'Ocon, Pilar,Fioravanti, Anna,Orlandi, Paola,Bocci, Guido,Dalla Via, Lisa
, p. 29 - 43 (2015/09/07)
Vascular Endothelial Growth Factor (VEGF) pathway has emerged as one of the most important positive modulators of Angiogenesis, a central process implicated in tumour growth and metastatic dissemination. This led to the design and development of anti-VEGF monoclonal antibodies and small-molecule ATP-competitive VEGFR-inhibitors. In this study, we describe the synthesis and the biological evaluation of novel 2-aryl substituted benzothiopyrano-fused pyrimidines 1a-i, 2a-i and 3a-i. The ability of the compounds to target the VEGF pathway was determined in vitro exploiting the compounds' antiproliferative efficacy against HUVEC cells. The VEGFR-2 inhibition was confirmed by enzymatic assays on recombinant human kinase insert domain receptor (KDR), by cell-based phospho-VEGFR-2 inhibition assays, and by ex vivo rat aortic ring tests. The selectivity profile of the best performing derivatives belonging to series 2 was further explored combining modeling studies and additional assays in a panel of human cell lines and other kinases.
Transition-metal-free approach to 4-ethynylpyrimidines via alkenynones
Golubev, Pavel R.,Pankova, Alena S.,Kuznetsov, Mikhail A.
, p. 3614 - 3621 (2014/06/23)
A practical approach to the synthesis of 4-ethynylpyrimidines by the condensation of arylamidines with 2-aryl-1-ethoxy-5-(trimethylsilyl)pent-1-en-4- yn-3-ones has been developed. As these latter ketones are easily accessible from bis(trimethylsilyl)acetylene and arylacetyl chlorides, the regioselective condensation reported herein provides a facile access to both TMS-protected and unprotected 4-ethynylpyrimidines in yields of up to 85%. Copyright
