Nicotinamide-based diamides derivatives as potential cytotoxic agents: synthesis and biological evaluation

作者：Peng, Min; Shi, Liqiao; Ke, Shaoyong^*

来源：Chemistry Central Journal, 2017, 11(1): 109.

DOI：10.1186/s13065-017-0338-5

• Nicotinamide
• Diamides
• Synthesis
• Lung cancer
• Cytotoxic activity

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-1 NMR, C-13 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 IC50 values of 4.07 +/- 1.30 mu g/mL, which might be developed as novel lead compounds for potential cytotoxic agents.

• 出版日期2017-10-24
• 单位湖北省农业科学院; 武汉大学