摘要/Abstract

经分子杂交技术[A1]合成了一系列4-取代-1-（2-甲基-6-（吡啶-3-基）-烟酰）氨基脲类衍生物.采用噻唑蓝（MTT）比色法研究了目标化合物对人肝癌细胞（QGY-7703）、人肺癌细胞（NCl-H460）和乳腺癌细胞（MCF-7）的体外抗肿瘤活性.1-（2-甲基-6-（吡啶-3-基）烟酰基）-4-（2，4，6-三氯苯基）氨基脲（4n）显示了最优的活性，其半数抑制浓度（IC₅₀）为8.89~11.45 μmol/L.细胞体内的生物研究显示，4n药物[A2]处理能明显增加细胞体内PARP切割水平以及诱导QGY-7703肿瘤细胞的凋亡.
关键词: 氨基脲, 联吡啶, 分子杂交, 生物活性
A series of 4-substitued-1-(2-methyl-6-(pyridin-3-yl)-nicotinoyl) semicarbazides were synthesized[A3] via molecular hybridization strategy. The synthesized compounds were screened for their anticancer potential against different cancer cells viz human hepatocelular carcinoma (QGY-7703), non-small cell lung (NCl-H460) and human breast (MCF-7) cancer cell lines by methyl thiazolyl tetrazolium (MTT) assay. 1-(2-Methyl-6-(pyridin-3-yl)nicotinoyl)-4-(2,4,6-trichlorophenyl)semicarbazide (4n) showed significant anticancer activity in these cancer cell lines with a range of IC₅₀ values from 8.89 μmol/L to 11.45 μmol/L. Further biology studies showed that 4n treatment obviously increased the level of cleaved PARP and induced the apoptosis in QGY-7703 cells.
Key words: semicarbazides, bipyridine, molecular hybridization, biological activity


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