879488-53-6Relevant academic research and scientific papers
Benzo-heterocycle substituted cyclopenta[4,5]pyrrolopyrazine-1-one derivatives and applications thereof
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Paragraph 0088-0090, (2019/10/04)
The invention relates to benzo-heterocycle substituted cyclopenta[4,5]pyrrolopyrazine-1-one derivatives, a preparation method of the same and applications of the same in medicinal use. Concretely, the invention discloses a compound of a formula (I), pharm
Copper-catalyzed selective C-N bond formation with 2-amino, 2-hydroxy and 2-bromo-5-halopyridine
Roy, Swarnali,Paul, Barnali,Mukherjee, Ayan,Kundu, Biswajit,Talukdar, Arindam
, p. 44366 - 44370 (2017/09/26)
A copper-catalyzed 1,2-diol amination at the electron-rich C-5 position of unprotected 2-amino/2-hydroxy-5-halopyridine provided excellent yields. Selective amination preferably at C-5 in 2-bromo-5-iodopyridine was achieved under the same conditions. The selective, generally mild and economical coupling reaction at C-5 position described herein could be achieved with amines, heterocycles and amides.
Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9
Rye, Carl S.,Chessum, Nicola E. A.,Lamont, Scott,Pike, Kurt G.,Faulder, Paul,Demeritt, Julie,Kemmitt, Paul,Tucker, Julie,Zani, Lorenzo,Cheeseman, Matthew D.,Isaac, Rosie,Goodwin, Louise,Boros, Joanna,Raynaud, Florence,Hayes, Angela,Henley, Alan T.,De Billy, Emmanuel,Lynch, Christopher J.,Sharp, Swee Y.,Te Poele, Robert,Fee, Lisa O',Foote, Kevin M.,Green, Stephen,Workman, Paul,Jones, Keith
supporting information, p. 1580 - 1586 (2016/08/24)
Heat shock factor 1 (HSF1) is a transcription factor that plays key roles in cancer, including providing a mechanism for cell survival under proteotoxic stress. Therefore, inhibition of the HSF1-stress pathway represents an exciting new opportunity in cancer treatment. We employed an unbiased phenotypic screen to discover inhibitors of the HSF1-stress pathway. Using this approach we identified an initial hit (1) based on a 4,6-pyrimidine scaffold (2.00 μM). Optimisation of cellular SAR led to an inhibitor with improved potency (25, 15 nM) in the HSF1 phenotypic assay. The 4,6-pyrimidine 25 was also shown to have high potency against the CDK9 enzyme (3 nM).
SUBSTITUTED BIPHENYL DERIVATIVE
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Page/Page column 167, (2010/11/27)
The present invention relates to a biaryl derivative or a pharmacologically acceptable salt thereof having an excellent collagen-synthesis inhibition activity. A biaryl derivative having a structure represented by the following General Formula (I) or a pharmacologically acceptable salt thereof: wherein R1 represents a C6-C10 aryl group which is substituted with one to three group(s) each independently selected from the group consisting of a group defined by formula R-L-, a di-(C1-C6 alkyl)amino group, a di-(C1-C6 alkyl)aminosulfonyl group, a hydroxyaminocarbonyl group, and a halogen atom, and so on; R represents a C1-C6 alkyl group, and so on; L represents a sulfonyl group, an aminosulfonyl group, or a sulfonylamino group, and so on; R2 represents a hydrogen atom, and so on; A represents a group defined by formula (II), (III), or (IV); R3 represents a C1-C6 alkyl group, and so on; and R4 represents a C1-C6 alkyl group, and so on.
