以1-[二(4-氟苯)甲基]哌嗪、溴丙炔及氯代肟为原料以21%~76%的收率制得了12个含有1-[4-二(4-氟苯)甲基哌嗪单元的异噁唑衍生物5a~5l.合成的12个目标化合物通过熔点测定和质谱、红外光谱、元素分析及核磁共振氢谱和碳谱分析对其结构进行确证.经体外抗肿瘤活性测试表明,在20μg/m L的浓度下,有10个化合物对细胞周期分裂蛋白25B(CDC25B)具有较好的抑制活性,其抑制率为64.15%~97.96%,IC_(50)为35.62~13.67μg/m L.在40μmol/L的浓度下,其中四个化合物对白血病HL-60细胞的IC_(50)为36.51~15.25μg/m L,2-(2-氟苯基)-5-(1-(二(4-氟苯)甲基)哌嗪)甲基异噁唑(5g),2-(2-氟苯基)-5-(1-(二(4-氟苯)甲基)哌嗪)甲基异噁唑(5h)对肺癌A-549肿瘤细胞的IC_(50)分别为21.09和35.36μg/m L.
【英文摘要】
Twelve novel isoxazoles containing(1-bi(4-fluorophenyl)methyl)piperazine unit were prepared in two steps starting from propargyl bromide,(1-bi(4-fluorophenyl)methyl)piperazine and hydroxymoyl chlorides with moderate yield(21%~76%). The structures of the new compounds were characterized by IR, MS, ~1H NMR, ~(13)C NMR and elemental analysis, and their in vitro anti-tumor activity was screened. The bioactive assay for the newly prepared compounds manifested that ten newly isoxazole derivatives exhibited good t...
【基金】
四川省科技厅科技支撑计划(No.2015NZ0033)资助项目~~
【更新日期】
2018-01-17
【分类号】
O626;TQ460.1
【正文快照】
*Corresponding author.E-mail:lqhchem@163.comReceived July 2,2017;revised August 19,2017;published online September 15,2017.Project supported by the Sichuan Provincial Department of Science and Technology Support Program(No.2015NZ0033).四川省科技厅科技支撑
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