140118-17-8Relevant articles and documents
Synthesis of 4-aryl and unsymmetrical 4,6-diarylpyrimidines by the Suzuki-Miyaura cross-coupling reaction
Gupta, Sahaj,Melanson, Jennifer A.,Selim Hossain,Vaillancourt, Louis,Tanoury, Gerald J.,Nugent, William A.,Snieckus, Victor
, p. 1549 - 1569 (2018/10/04)
A two-step procedure for the synthesis of 4-arylpyrimidines from inexpensive 4,6-dichloropyrimidine via a Suzuki-Miyaura/hydrodechlorination reaction sequence is described. The reaction resulted in the predominant formation of mono-arylated product. The c
Synthesis and evaluation of phosphorus containing, specific CDK9/CycT1 inhibitors
Németh, Gábor,Greff, Zoltán,Sipos, Anna,Varga, Zoltán,Székely, Rita,Sebestyén, Mónika,Jászay, Zsuzsa,Béni, Szabolcs,Nemes, Zoltán,Pirat, Jean-Luc,Volle, Jean-No?l,Virieux, David,Gyuris, ágnes,Kelemenics, Katalin,áy, éva,Minarovits, Janos,Szathmary, Susan,Kéri, Gy?rgy,Orfi, László
, p. 3939 - 3965 (2014/06/09)
Although there is a significant effort in the design of a selective CDK9/CycT1 inhibitor, no compound has been proven to be a specific inhibitor of this kinase so far. The aim of this research was to develop novel and selective phosphorus containing CDK9/CycT1 inhibitors. Molecules bearing phosphonamidate, phosphonate, and phosphinate moieties were synthesized. Prepared compounds were evaluated in an enzymatic CDK9/CycT1 assay. The most potent molecules were tested in cell-based toxicity and HIV proliferation assays. Selectivity of shortlisted compounds against CDKs and other kinases was tested. The best compound was shown to be a highly specific, ATP-competitive inhibitor of CDK9/CycT1 with antiviral activity.
(3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: Synthesis, in vitro, in vivo, and X-ray crystallographic characterization
Wright, Stephen W.,Ammirati, Mark J.,Andrews, Kim M.,Brodeur, Anne M.,Danley, Dennis E.,Doran, Shawn D.,Lillquist, Jay S.,Liu, Shenping,McClure, Lester D.,McPherson, R. Kirk,Olson, Thanh V.,Orena, Stephen J.,Parker, Janice C.,Rocke, Benjamin N.,Soeller, Walter C.,Soglia, Carolyn B.,Treadway, Judith L.,VanVolkenburg, Maria A.,Zhao, Zhengrong,Cox, Eric D.
, p. 5638 - 5642 (2008/02/13)
A series of pyrrolidine based inhibitors of dipeptidyl peptidase IV were developed from a high throughput screening hit for the treatment of type 2 diabetes. Potency, selectivity, and pharmacokinetic properties were optimized resulting in the identification of a pre-clinical candidate for further profiling.
SUBSTITUTED PYRIMIDIN-4-YLAMINA ANALOGUES AS VANILLOID RECEPTOR LIGANDS
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Page/Page column 47, (2008/06/13)
Substituted pyrimidyl-4-ylamine analogues are provided, of the Formula: (I) wherein variables are as described herein. Such compounds are ligands that may be used to modulate Vanilloid receptor activity in vivo or in vitro, and are particularly useful in
Pyrimidyl-substituted acrylic esters
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, (2008/06/13)
There are described new pyrimidyl-substituted acrylic esters of the general formula (I) STR1 in which Py, X, R1 and R2 have the meaning given in the description, a process for their preparation, and new intermediates. The compounds of the formula (I) are used as pesticides.