105602-45-7Relevant academic research and scientific papers
Synthesis and biological evaluation of 2,4-disubstituted thiazole amide derivatives as anticancer agent
Zhang, Zhi-Hua,Wu, Hong-Mei,Deng, Sai-Nan,Chai, Rui-Xia,Mwenda, Muriira Cyrus,Peng, Yuan-Yuan,Cai, Dong,Chen, Yu
, p. 355 - 364 (2019)
A series of novel 2,4-disubstituted thiazole amide derivatives were synthesized, and their antiproliferative activities were tested. Some of these compounds displayed good antiproliferative activity, especially for HT29 cell. Among these compounds, compound 5b inhibits A549, HeLa, HT29 and Karpas299 cells with IC50 values of 8.64, 6.05, 0.63 and 13.87?μM, respectively. The western blot analysis and docking study provide important clues for further optimization of compound 5b as a potential c-Met inhibitor.
Studies on Cerebral Protective Agents. VIII. Synthesis of 2-Aminothiazoles and 2-Thiazolecarboxamides with Anti-anoxic Activity
Okhubo, Mitsuru,Kuno, Atsushi,Nakanishi,Isao,Takasugi, Hisashi
, p. 1497 - 1504 (2007/10/03)
Various 2-aminothiazoles (2a-s and 3a-g) and 2-thiazolecarboxamides (4a-h), possessing a nitrogeneous basic moiety at the C-2 position of the thiazole ring, were prepared and tested for anti-anoxic (AA) activity in mice.Among them, N-4-(3-trifluoromethylphenyl)-2-thiazolecarbaxamide hydrochloride (4e, FR108143) (minimum effective doses of 3,2 mg/kg i.p. and 10 mg/kg p.o., respectively) exhibited more potent AA activity than either FK360 or compound 1, each of which has a nitrogeneous basic moiety at the C-5 position.The structure-activity relationship with regard to AA activity of this series of compounds are discussed, and the three-dimensional electrostatic potentials (3D-MEP) around the basic nitrogen atom of FK360 and the thiazole derivative (4e) are compared.Key words cerebral protective agent; anti-anoxia; 2-aminothiazole; 2-thiazolecarboxamide; structure-activity relationship; FK360
