18794-95-1Relevant articles and documents
Design, synthesis and anti-tumor evaluation of 1,2,4-triazol-3-one derivatives and pyridazinone derivatives as novel CXCR2 antagonists
Chu, Bizhu,Jiang, Yuyang,Li, Qinyuan,Liu, Zijian,Luo, Jingyi,Shi, Zhichao,Xin, Qilei,Ye, Lizhen,Zhan, Feng,Zhang, Xun,Zhu, Qingyun
, (2021/09/20)
Chemokine receptor 2 (CXCR2) is the receptor of glutamic acid–leucine–arginine sequence-contained chemokines CXCs (ELR+ CXCs). In recent years, CXCR2-target treatment strategy has come a long way in cancer therapy. CXCR2 antagonists could block
Discovery of novel 7-azaindole derivatives bearing dihydropyridazine moiety as c-Met kinase inhibitors
Tang, Qidong,Wang, Linxiao,Duan, Yongli,Wang, Wenhui,Huang, Shunmin,Zhi, Jia,Jia, Shuang,Zhu, Wufu,Wang, Ping,Luo, Rong,Zheng, Pengwu
, p. 97 - 106 (2017/04/07)
A series of 7-azaindole derivatives bearing the dihydropyridazine scaffold were synthesized and evaluated for their c-Met kinase inhibitory, and antiproliferative activity against 4 cancer cell lines (HT29, A549, H460, U87MG) were evaluated in?vitro. Most compounds showed moderate to excellent potency. Compared to foretinib, the most promising analog 34 (c-Met IC50: 1.06?nM, a multitarget tyrosine kinase inhibitor) showed a 6.4-, 7.8-, and 3.2-fold increase in activity against HT29, A549, and H460?cell lines, respectively. Structure activity relationship studies indicated that mono-EWGs (such as R2?=?F) at 4-position of moiety D was a key factor in improving the antitumor activity.
Microwave assisted synthesis and biological activity of 4-(2-(aryl substituted) hydrazono)-1-(2-(p-tolyloxyacetyl)-3-methyl-1H-pyrazol- 5-one
Jois, H.S. Vidyashree,Kalluraya, Balakrishna,Babu,Bhagya,Chandrashekar
, p. 7 - 10 (2019/01/21)
A novel series of 4-(2-(aryl substituted) hydrazono)-1-(2-(p-tolyloxy) acetyl)-3-methyl- 1H-pyrazol-5-ones 3(a-j) was prepared by the reaction of ethyl-2-arylhydrazono -3- oxobutyrate and p-tolyloxyacethydrazide under microwave irradiation. The structures of the synthesized compounds were established by their spectral and analytical data. All the new compounds were screened for their antibacterial and antifungal activity.