100137-20-0Relevant academic research and scientific papers
Glucokinase Activators Based on N-Aryl-N′-Pyridin-2-Ylurea Derivatives
Semenov,Tarasova,Khramov,Semenova,Inchina,Vakaeva
, p. 209 - 212 (2018)
A series of previously undescribed N-aryl-N′-pyridin-2-ylureas were prepared via the reaction of 2-aminopyridines with benzoyl azides and tested in vitro as activators of glucokinase. Statistically significant reductions of glucose levels as compared with
Design and Synthesis of Novel Thiazolo[5,4-d]pyrimidine Derivatives as Potential Angiogenesis Inhibitors
Xue, Wen-Jun,Du, Jian-Yao,Deng, Ya-Hui,Yan, Zhong-Hui,Liu, Ji-Ping,Liu, Yu,Sun, Li-Ping
, (2019/08/07)
Vascular endothelial growth factor receptor-2 (VEGFR-2) plays an important role in both vasculogenesis and angiogenesis. Inhibition of VEGFR-2 has been demonstrated as a key method against tumor-associated angiogenesis. Thiazolopyrimidine is an important analog of the purine ring, and we choose the thiazolopyrimidine scaffold as the mother nucleus. Two series of thiazolo[5,4-d]pyrimidine derivatives were synthesized and evaluated for their antiproliferative activity. In HUVEC inhibition assay, compounds 3l (=1-(5-{[2-(4-chlorophenyl)-5-methyl[1,3]thiazolo[5,4-d]pyrimidin-7-yl]amino}pyridin-2-yl)-3-(3,4-dimethylphenyl)urea) and 3m (=1-(5-{[2-(4-chlorophenyl)-5-methyl[1,3]thiazolo[5,4-d]pyrimidin-7-yl]amino}pyridin-2-yl)-3-(4-methoxyphenyl)urea) exhibited the most potent inhibitory effect (IC50=1.65 and 3.52 μm, respectively). Compound 3l also showed the best potency against VEGFR-2 at 50 μm (98.5 %). These results suggest that further investigation of compound 3l might provide potential angiogenesis inhibitors.
UREA SUBSTITUTED SULPHONAMIDE DERIVATIVES
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Page/Page column 57; 64-65, (2010/12/31)
The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially α2β1 integrin inhibitors e.g. in connection with diseases and
