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为了获取抗肿瘤活性化合物,通过拼合原理,设计合成了9个目标化合物,经IR、~1HNMR、~(13)CNMR及元素分析确认结构。采用溴化噻唑蓝四氮唑(MTT)法进行了抗肿瘤活性测试。结果表明,该类化合物对所测肿瘤细胞有增殖抑制作用,其中化合物Ⅲf、Ⅲi有较好抗肿瘤活性,尤以Ⅲi最为突出,对肿瘤细胞A-549、SGC-7901和EC-109均有显著抑制作用,IC50分别为(7.0±0.8)、(6.9±0.8)、(7.3±0.7)μmol/L,与对照药cisplatin相当。该类化合物值得进一步研究。
In order to obtain antitumor activity compounds, nine target compounds were designed and synthesized based on the principle of splitting. The structures were confirmed by IR, ~ 1HNMR, ~ (13) CNMR and elemental analysis. The anti-tumor activity was tested by MTT method. The results showed that these compounds had inhibitory effects on the proliferation of tumor cells. Among them, the compounds Ⅲf and Ⅲi had better anti-tumor activity, especially Ⅲi, and had the highest inhibitory effect on tumor cells A-549, SGC-7901 and EC-109 IC50 were (7.0 ± 0.8), (6.9 ± 0.8) and (7.3 ± 0.7) μmol / L respectively, which was comparable to the control drug cisplatin. Such compounds deserve further study.