753500-79-7Relevant academic research and scientific papers
Synthesis and bioevaluation study of novel N-methylpicolinamide and thienopyrimidine derivatives as selectivity c-Met kinase inhibitors
Wang, Linxiao,Xu, Shan,Chen, Xiuying,Liu, Xiaobo,Duan, Yongli,Kong, Dejia,Zhao, Dandan,Zheng, Pengwu,Tang, Qidong,Zhu, Wufu
, p. 245 - 256 (2018)
Four series of N-methylpicolinamide moiety and thienopyrimidine moiety bearing pyridazinone were designed and synthesized and evaluated for the IC50 values against three cancer cell lines (A549, HepG2 and MCF-7) and some selected compounds were
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.
Type II diabetes-related enzyme inhibition and molecular modeling study of a novel series of pyrazolone derivatives
Shetty, Shobhitha,Kalluraya, Balakrishna,Nithinchandra,Peethambar,Telkar, Sandeep B.
, p. 2834 - 2846 (2014/05/06)
Inhibitors of alpha-Amylase are targets for the development of novel drugs for the treatment of diabetes and obesity. Alpha amylase is an enzyme which increases the bio availability of glucose in the blood. Hence, the inhibition effects of alpha amylase of 2-[1-(4-isobutylphenyl)ethyl]-5-methyl-4-[2-(aryl- substituted)hydrazinylidene]-2,4-dihydro-3H-pyrazol-3-one (4a-l) were investigated, among them compounds 4d, 4f, 4a, and 4g have displayed good inhibitory activity. The compounds with significant results were further evaluated for their molecular modeling study using in silico method. The new series of compounds were synthesized by solvent-free microwave irradiation method and were characterized by spectral and analytical data.
Synthesis and pharmacological evaluation of pyrazolo[4,3-c]cinnoline derivatives as potential anti-inflammatory and antibacterial agents
Tonk, Rajiv Kumar,Bawa, Sandhya,Chawla, Gita,Deora, Girdhar Singh,Kumar, Suresh,Rathore, Vandana,Mulakayala, Naveen,Rajaram, Azad,Kalle, Arunasree M.,Afzal, Obaid
, p. 176 - 184 (2013/01/15)
A series of pyrazolo[4,3-c]cinnoline derivatives was synthesized, characterized and evaluated for anti-inflammatory and antibacterial activity. Test compounds that exhibited good anti-inflammatory activity were further screened for their ulcerogenic and l
