Wang, Qin; Rao, Nian; Liu, Li; Le, Yi; Yan, Longjia published the artcile< Development of 5-trifluoromethylpyrimidine derivatives as dual inhibitors of EGFR and SRC for cancer therapy>, Electric Literature of 112-63-0, the main research area is trifluoromethylpyrimidine derivative EGFR inhibitor antitumor mol docking.
In this paper, we reported a new series of 5-trifluoromethylpyrimidine derivatives (I [R = 4-methoxyphenyl, 2-fluorophenyl, 3-fluorophenyl, etc.], II [R = Pr, iso-Pr, hexyl, etc.]) for cancer therapy. They were tested for antitumor activity in vitro on four human cancer cell lines including A549, K562, HepG2, MCF-7 and two kinase including wild type epidermal growth factor receptor tyrosine kinase (EGFRwt-TK) and c-Src. The results suggested that some of the compounds (I [ R = 4-methoxyphenyl, 2-fluorophenyl, 3-fluorophenyl, 3,4-difluorophenyl], II [R = hexyl, Et acetate, iso-Pr, cyclopentyl, cyclohexyl, tetrahydropyran] 6b, 6d, 6e, 6f, 6g, 6h) performed well activities. Especially 2-((2-((4-((2-(Cyclohexylamino)-3,4-dioxocyclobut-1-en-1-yl)amino)phenyl)amino)-5-(trifluoro- methyl)pyrimidin-4-yl)amino)-N-methylbenzamide (6g) showed high antitumor activities against four cancer cell lines with 1.08 μM, 2.06 μM, 1.24 μM and 2.57 μM, resp. Furthermore, compound 2-((2-((4-((2-(cyclohexylamino)-3,4-dioxocyclobut-1-en-1-yl)amino)phenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)-N-methylbenzamide inhibited EGFRwt and Src at the values of 0.75 μM and 0.15 μM.
Heterocycles published new progress about Antitumor agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Electric Literature of 112-63-0.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics