The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: N5,N5-Dimethylpyridine-2,5-diamine( cas:39856-52-5 ) is researched.SDS of cas: 39856-52-5.Zhao, Hui; Hu, Xiaoxia; Cao, Kai; Zhang, Yue; Zhao, Kuantao; Tang, Chunlei; Feng, Bainian published the article 《Synthesis and SAR of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as potent and selective CDK4/6 inhibitors》 about this compound( cas:39856-52-5 ) in European Journal of Medicinal Chemistry. Keywords: pyrazoloquinazoline arylamino carboxamide preparation antitumor cyclin dependent kinase inhibitor; Anticancer; Cell cycle; Cyclin dependent kinase; Kinase selectivity. Let’s learn more about this compound (cas:39856-52-5).
CDK4/6 pathway is an attractive target for development of anti-cancer drugs. Herein, design and synthesis of a series of I (R1 = Ph; R2, R3 = H, Me; R4 = OEt, NH2, NHMe, NHEt) and I [R1 = 3-Me2NC6H4, 4-(piperazin-1-yl)phenyl, 2-pyridyl, etc.; R2 = R3 = H; R4 = NH2] as selective CDK4/6 inhibitors is reported. Applied with the optimizing strategy to the initial scaffold, it is found that the compound I [R1 = 5-(4-methylpiperazin-1-yl)pyridin-2-yl; R2 = R3 = H; R4 = NH2] is able to selectively inhibit CDK4 and CDK6 with IC50 values 0.01 and 0.026 μM, resp. This compound showed good anti-proliferative activity when tested in a panel of tumor cell lines with CDK4/6 related mechanism of action and worked much better than Ly2385219 which is a selective CDK4/6 inhibitor. This compound was also found to have favorable pharmacokinetic parameters.
I hope my short article helps more people learn about this compound(N5,N5-Dimethylpyridine-2,5-diamine)SDS of cas: 39856-52-5. Apart from the compound(39856-52-5), you can read my other articles to know other related compounds.