51119-05-2Relevant academic research and scientific papers
Design, synthesis and biological evaluation of sphingosine-1-phosphate receptor 2 antagonists as potent 5-FU-resistance reversal agents for the treatment of colorectal cancer
Luo, Dongdong,Zhang, Yuhang,Yang, Shuang,Tian, Xiaochen,Lv, Yan,Guo, Zhikun,Liu, Xiaochun,Han, Gaitian,Liu, Shuai,Wang, Wenyu,Cui, Shuxiang,Qu, Xianjun,Wan, Shengbiao
, (2021/08/20)
5-Fluorouracil (5-FU) and its prodrugs are the essential clinical drugs for colorectal cancer (CRC) treatment. However, the drug resistance of 5-FU has caused high mortality of CRC patients. Thus, it is urgent to develop reversal agents of 5-FU resistance. Sphingosine-1-phosphate receptor 2 (S1PR2) was proved to be a potential target for reversing 5-FU resistance, but the activity of known S1PR2 antagonists JTE-013 were weak in 5-FU-resistant cell lines. To develop more potent S1PR2 antagonists to treat 5-FU-resistant cancer, a series of JTE-013 derivatives were designed and synthesized. The most promising compound 40 could markedly reverse the resistance in 5-FU-resistant HCT116 cells and 5-FU-resistant SW620 cells via inhibiting the expression of dihydropyrimidine dehydrogenase (DPD). The key was that compound 40 with improved pharmacokinetic properties significantly increased the inhibitory rate of 5-FU in the SW620/5-FU cells xenograft model with no observable toxicity by inhibiting the expression of DPD in tumor and liver tissues. Altogether, these results suggest that compound 40 may be a promising drug candidate to reverse 5-FU resistance in the treatment of CRC.
Direct access to 2-aminopyrazolo[1,5-a]pyridines via N-amination/cyclization reactions of 2-pyridineacetonitriles
Nishigaya, Yosuke,Umei, Kentaro,Yamamoto, Eri,Kohno, Yasushi,Seto, Shigeki
supporting information, p. 5963 - 5966 (2014/12/11)
We describe the straightforward synthesis of 6-substituted-2-aminopyrazolo[1,5-a]pyridines from 2-pyridineacetonitriles by N-amination with O-(mesitylsulfonyl)hydroxylamine and subsequent base-promoted cyclization. This N-amination/intramolecular cyclization reaction allows access to a variety of 6-substituted-2-aminopyrazolo[1,5-a]pyridines in a one-pot procedure, in moderate to good yields.
PYRAZOLOPYRIDINE DERIVATIVE OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF
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Paragraph 0423; 0424, (2014/01/07)
A pyrazolopyridine derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof exhibits a strong EP1 receptor antagonistic effect. Thus, the derivative or the pharmacologically acceptable salt is useful as
