1023298-53-4Relevant articles and documents
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors
Huang, Xiaohua,Cheng, Cliff C.,Fischmann, Thierry O.,Duca, José S.,Richards, Matthew,Tadikonda, Praveen K.,Reddy, Panduranga Adulla,Zhao, Lianyun,Arshad Siddiqui,Parry, David,Davis, Nicole,Seghezzi, Wolfgang,Wiswell, Derek,Shipps Jr., Gerald W.
supporting information, p. 2590 - 2594 (2013/06/27)
Drug design efforts in the emerging 2-aminothiazole-4-carboxamide class of CHK1 inhibitors have uncovered specific combinations of key substructures within the molecule; resulting in significant improvements in cell-based activity while retaining a greater than one hundred-fold selectivity against CDK2. The X-ray crystal structure of a complex between compound 39 and the CHK1 protein detailing a 'U-shaped' topology and key interactions with the protein surface at the ATP site is also reported.
Discovery of a novel series of Chk1 kinase inhibitors with a distinctive hinge binding mode
Huang, Xiaohua,Cheng, Cliff C.,Fischmann, Thierry O.,Duca, Jose S.,Yang, Xianshu,Richards, Matthew,Shipps Jr., Gerald W.
supporting information; experimental part, p. 123 - 128 (2012/04/04)
A novel series of CHK1 inhibitors with a distinctive hinge binding mode, exemplified by 2-aryl-N-(2-(piperazin-1-yl)phenyl)thiazole-4-carboxamide, was discovered through high-throughput screening using the affinity selection-mass spectrometry (AS-MS)-based Automated Ligand Identification System (ALIS) platform. Structure-based ligand design and optimization led to significant improvements in potency to the single digit nanomolar range and hundred-fold selectivity against CDK2.
2-AMINOTHIAZOLE-4-CARBOXYLIC AMIDES AS PROTEIN KINASE INHIBITORS
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Page/Page column 83-84; 125-126, (2008/12/05)
The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.