60798-88-1Relevant academic research and scientific papers
Synthesis and antimicrobial activities of novel 6-(1,3-thiazol-4-yl)-1,3- benzoxazol-2(3H)-one derivatives
Laczkowski, Krzysztof Z.,Misiura, Konrad,Biernasiuk, Anna,Malm, Anna,Grela, Izabela
, p. 41 - 46 (2014/04/03)
Synthesis, characterization and investigation of antimicrobial activities of seven new 6-(1,3-thiazol-4-yl)-1,3-benzoxazol-2(3H)-ones are presented. Their structures were determined using 1H NMR, 13C NMR and elemental analyses. The compounds possess some biological activity against Gram-positive bacteria, especially against Micrococcus luteus belonging to opportunistic pathogens, with an MIC of 31.25 μg/mL.
Design, synthesis and biological evaluation of thiazolidinone derivatives as potential EGFR and HER-2 kinase inhibitors
Lv, Peng-Cheng,Zhou, Chang-Fang,Chen, Jin,Liu, Peng-Gang,Wang, Kai-Rui,Mao, Wen-Jun,Li, Huan-Qiu,Yang, Ying,Xiong, Jing,Zhu, Hai-Liang
experimental part, p. 314 - 319 (2010/04/02)
Two series of thiazolidinone derivatives designing for potential EGFR and HER-2 kinase inhibitors have been discovered. Some of them exhibited significant EGFR and HER-2 inhibitory activity. Compound 2-(2-(5-bromo-2-hydroxybenzylidene)hydrazinyl)thiazol-4(5H)-one (12) displayed the most potent inhibitory activity (IC50 = 0.09 μM for EGFR and IC50 = 0.42 μM for HER-2), comparable to the positive control erlotinib. Docking simulation was performed to position compound 12 into the EGFR active site to determine the probable binding model. Antiproliferative assay results indicating that some of the thiazolidinone derivatives own high antiproliferative activity against MCF-7. Compound 12 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent.
