Liu, Limin; Wang, Zhengjie; Gao, Chao; Dai, Honglin; Si, Xiaojie; Zhang, Yang; Meng, Yaqi; Zheng, Jiaxin; Ke, Yu; Liu, Hongmin; Zhang, Qiurong published the artcile< Design, synthesis and antitumor activity evaluation of trifluoromethyl-substituted pyrimidine derivatives>, SDS of cas: 611-19-8, the main research area is trifluoromethyl benzyl thio pyrimidin preparation SAR antitumor mol docking; Antitumor activity; Pyrimidine derivatives; Synthesis; Trifluoromethyl moiety.
In order to find efficient new antitumor drugs, a series of novel trifluoromethyl-substituted pyrimidine derivatives were designed and synthesized and the bioactivity against four human tumor cells (PC-3, MGC-803, MCF-7 and H1975) was evaluated by MTT assay. Compound I displayed potent anti-proliferative activity on H1975 (IC50 = 2.27 μM), which was better than the pos. control 5-FU (IC50 = 9.37 μM). Further biol. evaluation studies showed that compound I apoptosis of H1975 cells and arrested the cell cycle at G2/M phase. Furthermore, compound I induced H1975 cells apoptosis through increasing the expression of pro-apoptotic proteins Bax and p53 and down-regulating the anti-apoptotic protein Bcl-2. In addition, compound I was able to be tightly embedded in the active pocket of EGFR. These results demonstrated that compound I has a potential as a lead compound for further investigation.
Bioorganic & Medicinal Chemistry Letters published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 611-19-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2, SDS of cas: 611-19-8.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics