1366267-75-5Relevant academic research and scientific papers
Synthesis and Structure–Activity Relationship Study of Novel Pyrazolylthiazoles as Potential Anti-Breast Cancer Agents
Abbas, Eman M. H.,Dawood, Dina H.,Farghaly, Thoraya A.,El-hag, Fatma A.,Ali, Mamdouh M.
, p. 1974 - 1982 (2017)
A novel series of pyrazolylthiazole has been synthesized from the reaction of 5-(4-fluorophenyl)-3-aryl-4,5-dihydropyrazole-1-carbothioic acid amide derivatives with different reagents. The mechanism and structures of all the novel products were assured o
Design, synthesis and biological evaluation of pyrazolyl-thiazolinone derivatives as potential EGFR and HER-2 kinase inhibitors
Qiu, Ke-Ming,Wang, Hai-Hong,Wang, Li-Ming,Luo, Yin,Yang, Xian-Hui,Wang, Xiao-Ming,Zhu, Hai-Liang
experimental part, p. 2010 - 2018 (2012/05/04)
A series of pyrazolyl-thiazolinone derivatives (E1-E36) have been designed and synthesized and their biological activities were also evaluated as potential EGFR and HER-2 kinase inhibitors. Thirty-four of the 36 compounds were reported for the first time. Among them, compound 2-(5-(4-bromophenyl)-3-p-tolyl-4,5- dihydro-1H-pyrazol-1-yl)thiazol-4(5H)-one (E28) displayed the most potent inhibitory activity (IC50 = 0.24 μM for EGFR and IC50 = 1.07 μM for HER-2). Antiproliferative assay results indicated that compound E28 owned high antiproliferative activity against MCF-7, B16-F10 and HCT-116 in vitro, with IC50 value of 0.30, 0.54, and 0.70 μM, respectively. Docking simulation was further performed to position compound E28 into the EGFR active site to determine the probable binding model. Based on the preliminary results, compound E28 with potent inhibitory activity in tumor growth would be a potential anticancer agent.
