The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. It is also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Safety of 2,4-Dichloro-5-fluoropyrimidine.
Zhai, Zheng;Li, Ridong;Bai, Xinyu;Ning, Xianling;Lin, Zhiqiang;Zhao, Xuyang;Jin, Yan;Yin, Yuxin research published 《 Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors》, the research content is summarized as follows. A series of diphenylaminopyrimidine derivativesbearing dithiocarbamate moieties I [R = methylamino, N-pyrrolidinyl, benzylamino, etc.] and II [n = 1, 2, 3, 4; R1 = prop-2-enoyl, propanoyl; R2 = N,N-dimethylamino, 4-isopropylpiperazin-1-yl, 3-pyridinylmethylamino] were designed and synthesized as novel BTK inhibitors for treatment of B-cell lymphoma. Among all these compounds, compound I [R = 3-pyridinylmethylamino] (IC50 = 1.15 ± 0.19 nM) displayed similar or more potent inhibitory activity against BTK than spebrutinib (IC50 = 2.12 ± 0.32 nM) and FDA approved drug ibrutinib (IC50 = 3.89 ± 0.57 nM), which was attributed to close binding of compound I [R = 3-pyridinylmethylamino] with BTK predicted by mol. docking. In particular, compound I [R = 3-pyridinylmethylamino] exhibited enhanced anti-proliferative activity against B-lymphoma cell lines at the IC50 concentration of 0.357 ± 0.02 μM (Ramos) and 0.706 ± 0.05 μM (Raji), resp., almost 10-fold better than ibrutinib and spebrutinib. In addition, compound I [R = 3-pyridinylmethylamino] displayed stronger selectivity on B-cell lymphoma over other cancer cell lines than spebrutinib. Furthermore, compound I [R = 3-pyridinylmethylamino] efficiently blocks BTK downstream pathways and results in apoptosis of cancer cells. In-vivo xenograft model evaluation demonstrated the significant efficacy and broad safety margin of compound I [R = 3-pyridinylmethylamino] in treatment of B-cell lymphoma. Author propose that compound compound I [R = 3-pyridinylmethylamino] is a candidate for further study and development based on our current findings.
Safety of 2,4-Dichloro-5-fluoropyrimidine, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia