《Synthesis and biological evaluation of aurora kinases inhibitors based on N-trisubstituted pyrimidine scaffold》 was written by Long, Liang; Luo, Yu; Hou, Zhi-Jie; Ma, Hua-Juan; Long, Zi-Jie; Tu, Zheng-Chao; Huang, Lin-Jie; Liu, Quentin; Lu, Gui. Formula: C4HCl3N2This research focused ontrisubstituted pyrimidine preparation aurora kinase inhibitor antitumor human SAR; Anticancer drug; Aurora kinase inhibitor; Leukemia; N-trisubstituted pyrimidines; Synthesis. The article conveys some information:
The inhibition of the members of aurora kinase family using ATP-competitive small mols. was an effective method for anticancer therapeutics. Based on this concept, synthesis of new N-trisubstituted pyrimidine derivatives I [Ar = 4-FC6H4, 3-F-4-CO2MeC6H3, 3,4,5-MeO3C6H2, etc.] and evaluation of their biol. activities and stabilities were done. Among them, compound I [Ar = 3-Cl-4-FC6H3] showed the best inhibition against aurora A kinase (IC50 = 7.1 nM), human leukemia cell line U937 (IC50 = 12.2 nM) and the growth of U937 xenograft tumors in vivo. By flow cytometry and immunofluorescence anal. of U937, it was found that compound I [Ar = 3-Cl-4-FC6H3] could induced polyploidy formation including (4N, 8N and 16N) and induced defects in both chromosome alignment and spindle formation. Furthermore, compound I [Ar = 3-Cl-4-FC6H3] exhibited good chem., phys., and thermal stabilities. All these results suggested that compound I [Ar = 3-Cl-4-FC6H3] was a promising lead compound for further development of anticancer drugs.2,4,6-Trichloropyrimidine(cas: 3764-01-0Formula: C4HCl3N2) was used in this study.
2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. They are generally not present in crude oils and are typically the result of additives, cleaning solutions or chemicals used for oil recovery.Formula: C4HCl3N2
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia