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设计合成含有苯并噻唑及嘧啶并噻唑母核的化合物,评价其对信号转导及转录激活因子3(STAT3)信号转导通路的影响.以实验室前期报道的化合物16v为先导物,通过基于结构的药物设计及生物电子等排原理设计两个系列化合物.采用Luciferase法检测化合物对STAT3信号转导通路的影响.合成21个未见文献报道的新化合物,其结构经核磁共振氢谱、碳谱和质谱确证;Luciferase实验表明,苯并噻唑类部分化合物在10μmol·L-1浓度下能够很好的抑制IL-6刺激的STAT3信号转导通路,而嘧啶并噻唑类化合物活性较弱.
The compounds containing benzothiazole and pyrimidothiazole core were designed and synthesized to evaluate their effects on the signal transducer and activator of transcription 3 (STAT3) signal transduction pathway.According to the previously reported compound 16v in the laboratory, Structure design and bioisosterism principle, two series of compounds were designed.The effects of compounds on STAT3 signal transduction pathway were determined by Luciferase method.Twenty-one new compounds were synthesized and their structures were confirmed by 1H NMR, The results of Luciferase assay showed that some compounds of benzothiazole could inhibit the STAT3 signal transduction pathway stimulated by IL-6 at a concentration of 10μmol·L-1, but the activity of pyrimidothiazole compounds was weak.