N-乙酰基吡唑啉衍生物和二苯醚基N-乙酰基双吡唑啉衍生物的合成及体外抗肿瘤活性

Syntheses and in vitro Antitumor Activities of N-Acetyl Pyrazolines and Diphenyl Etheryl N-Acetyl Bis-pyrazolines

合成了7个N-乙酰基吡唑啉化合物2a^2g和7个新型的二苯醚基N-乙酰基双吡唑啉化合物4a^4g,通过核磁共振谱、元素分析和质谱对合成化合物进行了结构表征.并且用3-(4,5-二甲基吡啶-2-基)-5-(3-羧基甲氧基苯基)-2-(4-磺苯基)-2H-四唑(MTS)法测试了它们对人肺腺癌细胞(A549)、人非小细胞肺癌细胞(H1299)和乳癌细胞(MCF-7)三类癌细胞株的体外抗肿瘤活性.结果显示,所合成的化合物对癌细胞有一定抑制作用,其中3,3'-(4,4'-二苯醚基)双[1-乙酰基-5-(3,4-亚甲基二氧苯基)-2-吡唑啉](4e)对A549,H1299和MCF-7三类癌细胞株具有较好的抗肿瘤活性,半数抑制浓度(IC50)分别为16.91,10.09,10.97μmol/L.

Seven N-acetyl pyrazolines 2a-2g and seven N-acetyl bis-pyrazolines 4a-4g with diphenyl etheryl moiety were synthesized and characterized by ^1H NMR,^13C NMR, elemental analysis and ESI-MS, and their in vitro antitumor activities on A549, H1299 and MCF-7 were evaluated by 3-（4,5-dimethylthiazol-2-yl）-5-（3-carboxymethoxyphenyl）-2-（4-sulfophenyl-2Htetrazolium）（MTS） assay. The results showed those compounds exhibited potent antiproliferative effects on cancer cells, among them compound 3,3＇-（4,4＇-diphenyl ether）-5,5＇-bi[1-acetyl-5-（benzo[d][1,3]dioxo-5-yl）-2-pyrazoline]（4e） showed significantly inhibited the growth of all three kinds of cancer cells, the IC50 values of A549, H1299 and MCF-7 were 16.91, 10.09,10.97 μmol/L, respectively.