Liu, Limin published the artcileDesign, synthesis and antitumor activity evaluation of trifluoromethyl-substituted pyrimidine derivatives, Application of 1-(Chloromethyl)-4-(trifluoromethyl)benzene, the publication is Bioorganic & Medicinal Chemistry Letters (2021), 128268, database is CAplus and MEDLINE.
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 939-99-1. 939-99-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzyl chloride,Benzene, name is 1-(Chloromethyl)-4-(trifluoromethyl)benzene, and the molecular formula is C8H6ClF3, Application of 1-(Chloromethyl)-4-(trifluoromethyl)benzene.
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