173064-29-4Relevant articles and documents
Synthesis of novel substituted pyrimidine derivatives bearing a sulfamide group and their in vitro cancer growth inhibition activity
Lefebvre, Carole-Anne,Forcellini, Elsa,Boutin, Sophie,C?té, Marie-France,C.-Gaudreault, René,Mathieu, Patrick,Lagüe, Patrick,Paquin, Jean-Fran?ois
supporting information, p. 299 - 302 (2016/12/27)
The synthesis of two series of novel substituted pyrimidine derivatives bearing a sulfamide group have been described and their in vitro cancer growth inhibition activities have been evaluated against three human tumour cell lines (HT-29, M21, and MCF7). In general, growth inhibition activity has been enhanced by the introduction of a bulky substituent on the aromatic ring with the best compound having GI50??6?μM for all the human tumour cell lines. The MCF7 selective compounds were evaluated on four additional human invasive breast ductal carcinoma cell lines (MDA-MB-231, MDA-MB-468, SKBR3, and T47D) and were selective against T47D cell line in all cases except one, suggesting a potential antiestrogen activity.
SUBSTITUTED PYRIMIDINE COMPOUNDS AND USES THEREOF
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Page/Page column 68, (2014/01/07)
The present invention relates to pyrimidine compounds, (the compounds of formula 1), in all its stereoisomeric and tautomeric forms and mixtures thereof in all ratios; and their pharmaceutically acceptable salts, solvates, prodrugs and polymorphs and N-ox
(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.