Zhou, Haiping; Jiang, Junhao; Lu, Jinyu; Ran, Dongzhi; Gan, Zongjie published the artcile< Synthesis and biological evaluation of novel 2,4-dianilinopyrimidine derivatives as potent dual janus kinase 2 and histone deacetylases inhibitors>, Product Details of C7H4BrF3, the main research area is dianilinopyrimidine preparation janus kinase histone deacetylase inhibitor antitumor docking; tert butyl chloro pyrimidinyl amino benzenesulfonamide preparation; phenyl bromide chloro pyrimidinyl amine Buchwald Hartwig.
Herein, a novel series of 2,4-dianilinopyrimidine derivatives, I [R1 = 3-SO2NHC(CH3)3, 3-F, 3-SO2NHCH(CH3)2, etc.; R2 = H, Me; n = 0, 3, 5, 6] was presented which could simultaneously inhibit JAK2 and HDAC1. Among which, I [R1 = 3-OMe, R2 = Me, n = 6] was found to be the most potent compound and displayed balanced inhibitory activity against HDAC1 (IC50 = 1.9 nM) and JAK2 (IC50 = 0.5 nM), resp. [R1 = 3-OMe, R2 = Me, n = 6] also demonstrated good antiproliferative activity against tested cancer cell lines (A549, HepG-2, MDA-MB-231 and Jurkat). Moreover, flow cytometric anal. showed that I [R1 = 3-OMe, R2 = Me, n = 6] induced apoptosis and cell cycle arrest in a dose-dependent manner, and the insight into mechanisms of I [R1 = 3-OMe, R2 = Me, n = 6] indicated that it could decrease the phosphorylation of STAT-3 and promote histone acetylation. In conclusion, these results together suggested that I [R1 = 3-OMe, R2 = Me, n = 6] would be a promising lead candidate and deserved further research and development.
Journal of Molecular Structure published new progress about Antiproliferative agents. 401-78-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3, Product Details of C7H4BrF3.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary