- Synthesis of novel substituted pyrimidine derivatives bearing a sulfamide group and their in vitro cancer growth inhibition activity
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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.
- Lefebvre, Carole-Anne,Forcellini, Elsa,Boutin, Sophie,C?té, Marie-France,C.-Gaudreault, René,Mathieu, Patrick,Lagüe, Patrick,Paquin, Jean-Fran?ois
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supporting information
p. 299 - 302
(2016/12/27)
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- Synthesis and evaluation of phosphorus containing, specific CDK9/CycT1 inhibitors
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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.
- 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
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p. 3939 - 3965
(2014/06/09)
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- SUBSTITUTED PYRIMIDINE COMPOUNDS AND USES THEREOF
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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
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Page/Page column 68
(2014/01/07)
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- 4, 6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES AS INHIBITORS OF PROTEIN KINASES
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The present invention relates to inhibitors of general Formula (I) of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to compounds for preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases.
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Page/Page column 160; 174
(2008/12/08)
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- (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
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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.
- 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.
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p. 5638 - 5642
(2008/02/13)
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- Synthesis of unsymmetrical 4,6-diarylpyrimidines
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Unsymmetrical 4,6-diarylpyrimidines were synthesized using Suzuki coupling reaction via selective arylation of 4,6-dichloropyrimidine.
- Zhou, Bishan,Taylor, Brett,Kornau, Kathryn
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p. 3977 - 3979
(2012/08/29)
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