771-81-3Relevant academic research and scientific papers
A synthetic DNA - PK inhibitors STL127705 method (by machine translation)
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Paragraph 0035; 0039; 0041, (2019/10/04)
The invention discloses a method for synthesizing DNA - PK inhibitors STL127705 method. This invention adopts the retrosynthetic analysis, in order to 2 - sulfide - 4 - chloro pyrimidine - 5 - carboxylic acid ethyl ester as the starting material, successi
Pyridopyrimidinone derivatives as potent and selective c-jun N-terminal kinase (JNK) inhibitors
Zheng, Ke,Park, Chul Min,Iqbal, Sarah,Hernandez, Pamela,Park, Hajeung,Lograsso, Philip V.,Feng, Yangbo
supporting information, p. 413 - 418 (2015/04/27)
A novel series of 2-aminopyridopyrimidinone based JNK (c-jun N-terminal kinase) inhibitors were discovered and developed. Structure-activity relationships (SARs) were systematically developed utilizing biochemical and cell based assays and in vitro and in vivo drug metabolism and pharmacokinetic (DMPK) studies. Through the optimization of lead compound 1, several potent and selective JNK inhibitors with high oral bioavailability were developed. Inhibitor 13 was a potent JNK3 inhibitor (IC50 = 15 nM), had high selectivity against p38 (IC50 > 10 μM), had high potency in functional cell based assays, and had high stability in human liver microsome (t1/2 = 76 min), a clean CYP-450 inhibition profile, and excellent oral bioavailability (%F = 87). Moreover, cocrystal structures of compounds 13 and 22 in JNK3 were solved at 2.0 ?. These structures elucidated the binding mode (Type-I binding) and can pave the way for further inhibitor design of this pyridopyrimidinone scaffold for JNK inhibition.
NOVEL COMPOUNDS AS JNK KINASE INHIBITORS
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Page/Page column 93, (2015/06/18)
The present invention is directed to modulators, such as inhibitors, of JNK isoform 2 (JNK2) or isoform 3 (JNK3) comprising compounds of formula (I) or formula (II) as described herein. Compounds of the invention can be used for treatment of a medical dis
P-38 kinase inhibitors
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Page/Page column 27, (2008/06/13)
Compounds and compositions for modulating the activity of p38 kinases are provided, including p38α and p38β kinase. Methods for treating, preventing or ameliorating one or more symptoms of a p38 kinase mediated disease or disorder are also provided.
