Derivatives of 5-nitro-1H-benzo[de]isoquinoline-1,3(2H)-dione: design, synthesis, and biological activity |
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Authors: | Aibin Wu Jide Liu Shaoxiong Qin and Ping Mei |
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Institution: | (1) College of Chemistry and Environmental Engineering, Yangtze University, 434023 Jingzhou, People’s Republic of China |
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Abstract: | Abstract A series of mono and bis-2-(2-(dimethylamino)-ethyl)-5-nitro-1H-benzode]isoquinoline-1,3(2H)-diones with different amino side chains, a novel family of antitumor agents, has been designed and synthesized. Their antitumor
activity was evaluated against HeLa, A549, P388, HL-60, MCF-7, HCT-8, and A375 cancer cell lines in vitro. Preliminary results
showed that most of the derivatives had antitumor activity comparable with that of mitonafide, with IC
50 values of 10−6–10−5 M. More importantly, the derivatives had distinct antitumor selectivity against different cancer cell lines. This work provided
a novel class of mitonafide-based lead compounds with improved antitumor selectivity against cancer cell lines for further
optimization. |
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Keywords: | |
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