Peng Min, Shi Liqiao, Ke Shaoyong
Department of Oncology, Renmin Hospital of Wuhan University, Wuhan University, Wuhan, 430060, Hubei, China.
National Biopesticide Engineering Technology Research Center, Hubei Academy of Agricultural Sciences, Wuhan, 430064, China.
Chem Cent J. 2017 Oct 24;11(1):109. doi: 10.1186/s13065-017-0338-5.
A series of diamides derivatives containing nicotinamide unit were designed, synthesized and evaluated for their potential cytotoxic activities against human cancer cell lines. All the synthesized compounds were characterized using spectroscopic methods mainly including H NMR, C NMR and MS. The bio-evaluation results indicated that some of the obtained compounds (such as 4d, 4h, 4i) exhibited good to moderate cytotoxic effects on lung cancer cell lines (NCI-H460, A549, and NCI-H1975), especially, compound 4d exhibited the highly potential inhibitory activities against NCI-H460 cell line with the IC values of 4.07 ± 1.30 μg/mL, which might be developed as novel lead compounds for potential cytotoxic agents.
设计、合成了一系列含烟酰胺单元的二酰胺衍生物，并评估了它们对人癌细胞系的潜在细胞毒活性。所有合成的化合物均采用光谱方法进行表征，主要包括氢核磁共振（¹H NMR）、碳核磁共振（¹³C NMR）和质谱（MS）。生物评价结果表明，部分所得化合物（如4d、4h、4i）对肺癌细胞系（NCI-H460、A549和NCI-H1975）表现出良好至中等程度的细胞毒作用，尤其是化合物4d对NCI-H460细胞系表现出高度潜在的抑制活性，其半数抑制浓度（IC）值为4.07±1.30μg/mL，有望开发成为新型潜在细胞毒药物的先导化合物。
