Introduction of a new synthetic route about 60748-47-2

《Synthesis and biological evaluation of novel 2,4-dianilinopyrimidine derivatives as potent dual janus kinase 2 and histone deacetylases inhibitors》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(PD2DBA3)Application of 60748-47-2.

Application of 60748-47-2. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: PD2DBA3, is researched, Molecular C51H42O3Pd2, CAS is 60748-47-2, about Synthesis and biological evaluation of novel 2,4-dianilinopyrimidine derivatives as potent dual janus kinase 2 and histone deacetylases inhibitors. Author is Zhou, Haiping; Jiang, Junhao; Lu, Jinyu; Ran, Dongzhi; Gan, Zongjie.

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.

《Synthesis and biological evaluation of novel 2,4-dianilinopyrimidine derivatives as potent dual janus kinase 2 and histone deacetylases inhibitors》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(PD2DBA3)Application of 60748-47-2.

Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method