5626-85-7Relevant academic research and scientific papers
Identification of pyrimidine derivatives as hSMG-1 inhibitors
Gopalsamy, Ariamala,Shi, Mengxiao,Bennett, Eric M.,Bard, Joel,Zhang, Wei-Guo,Yu, Ker
, p. 6636 - 6641,6 (2012/12/12)
hSMG-1 kinase plays a dual role in a highly conserved RNA surveillance pathway termed nonsense-mediated RNA decay (NMD) and in cellular genotoxic stress response. Since deregulation of cellular responses to stress contributes to tumor growth and resistance to chemotherapy, hSMG-1 is a potential target for cancer treatment. From our screening efforts, we have identified pyrimidine derivatives as hSMG-1 kinase inhibitors. We report structure-based optimization of this pan-kinase scaffold to improve its biochemical profile and overall kinome selectivity, including mTOR and CDK, to generate the first reported selective hSMG-1 tool compound.
PYRIMIDINE SULFONAMIDE ANALOGS AND THEIR USE AS AGONISTS OF THE WNT-BETA-CATENIN CELLULAR MESSAGING SYSTEM
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Page/Page column 14, (2009/03/07)
The present invention relates to pyrimidine sulfonamide analogs, methods of making pyrimidine sulfonamide analogs, compositions comprising a pyrimidine sulfonamide analog, and methods for treating canonical Wnt-β-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of a pyrimidine sulfonamide analog.
Anilino-pyrimidine analogs
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Page/Page column 22, (2010/10/20)
The present invention relates to compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are defined herein.
IMIDAZO[1,2-A]PYRIDINE AND PYRAZOLO[2,3-A]PYRIDINE DERIVATIVES
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Page/Page column 40, (2010/02/04)
A compound of formula (I) wherein Ring A is imidazol[1,2a]pyrid-3-yl or pyrazolo[2,3a]pyrid-3-yl; Ris as defined within; m is 0-5; wherein the values of Rmay be the same or different; Ris as defined within; n is 0 to 2, wherein the values of Rmay be the same or different; Ring B is phenyl or phenyl fused to a C5-7cycloalkyl ring; Ris as defined within; p is 0-4; wherein the values of Rmay be the same or different; Ris as defined within; q is 0-2; wherein the values of Rmay be the same or different; and wherein p+q=5; or a pharmaceutically acceptable salt or an in vivo hydrolyzable ester thereof is described. The use of compounds of formula (I) in the inhibition of cell cycle kinases CDK2, CDK4, and CDK6 are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.
Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
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, (2008/06/13)
The present invention provides compounds of formula I: wherein G is a small group selected from hydrogen or C1-3 alkyl, Q is pyridine or pyrimidine, and R1-R3 are as defined in the specification. These compounds are select
