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将天然产物apicidin分子中大环结构简化,并对锌离子结合区结构修饰,设计了两类取代乙酸己(庚)硫酯类化合物。所合成的26个化合物结构经1H NMR、IR、MS与HR-MS确证。采用MTT法与台盼蓝染色法对目标化合物进行了体外抗肿瘤活性筛选,药理结果显示,化合物II-1、II-3、II-6、II-13针对HL-60肿瘤细胞活性较好,IC50值达到微摩尔级,化合物II-7、II-8针对MCF-7肿瘤细胞的抑制作用优于阳性对照药伏立诺他,IC50值分别为3.19和6.29μmol·L-1。
The macrocyclic structures of apicidin, a natural product, were simplified and two kinds of substituted hexyl (heptyl) thioesters were designed for the structural modification of zinc ion binding sites. The structures of the 26 compounds synthesized were confirmed by 1H NMR, IR, MS and HR-MS. The target compounds were screened by MTT assay and trypan blue staining in vitro. The pharmacological results showed that the compounds II-1, II-3, II-6 and II-13 have good activity against HL-60 tumor cells, The IC50 values reached micromolar. The inhibitory effect of compounds II-7 and II-8 on MCF-7 tumor cells was better than that of vinorelbine with IC50 values of 3.19 and 6.29μmol·L-1, respectively.