Synthesis and Biological Evaluation of Novel Acenaphthene Derivatives as Potential Antitumor Agents
Abstract
:1. Introduction
2. Results and Discussion
2.1. Chemistry
2.2. Antiproliferative Activities
3. Experimental
3.1. General
3.2. Preparation of 5-Bromoacetylacenaphthene (1)
3.3. General Procedure for Preparing Compounds 3a-h
3.4. General Procedure for Preparing Compounds 4a-d
3.5. Cell Culture
3.6. Cell Proliferation Assay (MTT Assay)
4. Conclusions
Acknowledgements
References
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Sample Availability: Samples are available from the authors. |
Compd. | R1 | R2 | Inhibition rate (%) | |||||
---|---|---|---|---|---|---|---|---|
H460 | SW480 | MDA-MB-468 | SKRB-3 | A375 | BxPC-3 | |||
3a | -NH2 | - | 25.2±2.8 | 1.7±2.3 | 0.8±3.9 | 1.3±8.8 | 42.3±2.2 | 4.0±3.4 |
3b | - | 19.3±6.6 | 20.2±5.6 | 27.3±6.8 | 35.2±3.2 | 25.7±3.2 | 18.6±2.8 | |
3c | - | 24.3±9.1 | 22.6±3.0 | 55.5±3.8 | 66.1±2.2 | 31.7±5.0 | 17.1±3.7 | |
3d | - | 12.2±4.0 | 11.1±2.5 | 31.6±8.1 | 42.4±2.9 | 18.2±9.2 | 6.1±5.5 | |
3e | - | 20.6±5.2 | 0.4±2.6 | 15.2±7.3 | 20.7±4.4 | 0.5±1.5 | 2.6±6.6 | |
3f | - | 33.8±1.6 | 30.7±0.5 | 25.9±1.5 | 47.5±2.8 | 10.5±1.0 | 20.6±2.4 | |
3g | - | 26.2±2.1 | 1.9±2.6 | 5.2±3.7 | 34.7±6.6 | 4.9±3.1 | 1.1±7.8 | |
3h | - | 43.7±1.3 | 41.1±2.7 | 30.6±0.6 | 41.6±2.4 | 9.1±1.6 | 32.1±1.0 | |
4a | - | 12.1±0.5 | 14.6±1.4 | 20.5±1.6 | 31.0±4.8 | 22.6±2.5 | 10.2±1.7 | |
4b | - | 17.6±0.8 | 33.8±4.0 | 31.3±1.3 | 41.7±5.2 | 35.0±6.6 | 20.2±1.4 | |
4c | - | 19.3±3.2 | 16.3±0.4 | 13.2±5.0 | 26.3±3.0 | 16.6±7.1 | 11.4±3.6 | |
4d | - | 35.1±3.3 | 22.7±1.0 | 25.3±1.9 | 38.0±2.8 | 39.7±1.9 | 25.0±3.5 | |
ADM | - | - | 63.3±0.9 | 46.1±0.4 | 63.4±0.4 | 68.1±1.3 | 70.4±2.0 | 39.4±0.7 |
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Xie, Y.-M.; Deng, Y.; Dai, X.-Y.; Liu, J.; Ouyang, L.; Wei, Y.-Q.; Zhao, Y.-L. Synthesis and Biological Evaluation of Novel Acenaphthene Derivatives as Potential Antitumor Agents. Molecules 2011, 16, 2519-2526. https://doi.org/10.3390/molecules16032519
Xie Y-M, Deng Y, Dai X-Y, Liu J, Ouyang L, Wei Y-Q, Zhao Y-L. Synthesis and Biological Evaluation of Novel Acenaphthene Derivatives as Potential Antitumor Agents. Molecules. 2011; 16(3):2519-2526. https://doi.org/10.3390/molecules16032519
Chicago/Turabian StyleXie, Yong-Mei, Yi Deng, Xiao-Yun Dai, Jie Liu, Liang Ouyang, Yu-Quan Wei, and Ying-Lan Zhao. 2011. "Synthesis and Biological Evaluation of Novel Acenaphthene Derivatives as Potential Antitumor Agents" Molecules 16, no. 3: 2519-2526. https://doi.org/10.3390/molecules16032519