1-取代苄基-4-[1-(二-(4-氟苯)甲基)哌嗪甲基]-1H-1,2,3-三氮唑衍生物的设计合成及抗肿瘤活性研究

Design,synthesis and anti-tumor evaluation of 1-substituted benzyl-4-[4-bi-(1.4-fluorophenyl) methyl-piperazin-1-yl-methyl]-1,2,3-triazole derivatives

以1-[二-(4-氟苯)甲基]哌嗪为原料,CuBr_2为催化剂,DMF-H_2O为溶剂,经Click反应4h,以46-83%的收率制得了6个含1-[4-二-(4-氟苯)甲基]哌嗪基官能团的1,2,3-三氮唑衍生物3(a^f).其结构均经红外、质谱、核磁共振氢谱和碳谱所确证.并进行了体外抗肿瘤活性测试.测试表明有4个化合物对CDC25B具有较好的抑制活性,其抑制率高达86.30%,IC_(50)可高达6.68μg/mL.

Six novel 1,2,3-triazole derivatives 3（a^f） were prepared by Click reaction using bi-（4-fluorophenyl）methylchloro as starting material, copper（II） bromide as catalyst and DMF-H2O （1：1） as solvent for 4h with good yield （46-83%）. The structures of the new 1,2,3-triazole compounds were confirmed by IR, MS, 1H NMR, and 13C NMR. The bioactive assay for the newly prepared compounds manifested that four 1,2,3-triazole derivatives exhibited good inhibitory activity against CDC25B （Inhibition rate up to 86.30%, IC50 value up to 6.68. ug/mL）.