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Molecules 2016, 21(5), 530; doi:10.3390/molecules21050530

Novel N-Substituted 2-(2-(Adamantan-1-yl)-1H-Indol-3-yl)-2-Oxoacetamide Derivatives: Synthesis and Biological Evaluation

School of Pharmaceutical Sciences and the Key Laboratory for Chemical Biology of Fujian Province, Xiamen University, South Xiang-An Road, Xiamen 361102, China
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 7 March 2016 / Revised: 3 April 2016 / Accepted: 16 April 2016 / Published: 5 May 2016
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In this study, a series of novel N-substituted 2-(2-(adamantan-1-yl)-1H-indol-3-yl)-2-oxoacetamide derivatives were synthesized, and evaluated for their cytotoxicity in human cell lines including Hela (cervical cancer), MCF7 (breast cancer ) and HepG2 (liver cancer). Several compounds were found to have potent anti-proliferative activity against those human cancer cell lines and compound 5r showed the most potent biological activity against HepG2 cells with an IC50 value of 10.56 ± 1.14 μΜ. In addition, bioassays showed that compound 5r induced time-dependent and dose-dependent cleavage of poly ADP-ribose polymerase (PARP), and also induced a dose-dependent increase in caspase-3 and caspase-8 activity, but had little effect on caspase-9 protease activity in HepG2 cells. These results provide evidence that 5r-induced apoptosis in HepG2 cell is caspase-8-dependent. View Full-Text
Keywords: 2-(2-(adamantan-1-yl)-1H-indol-3-yl)-2-oxoacetamidederivatives; poly ADP-ribose polymerase (PARP); caspase-8; apoptosis 2-(2-(adamantan-1-yl)-1H-indol-3-yl)-2-oxoacetamidederivatives; poly ADP-ribose polymerase (PARP); caspase-8; apoptosis

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Hu, H.-Y.; Yu, X.-D.; Wang, F.; Lin, C.-R.; Zeng, J.-Z.; Qiu, Y.-K.; Fang, M.-J.; Wu, Z. Novel N-Substituted 2-(2-(Adamantan-1-yl)-1H-Indol-3-yl)-2-Oxoacetamide Derivatives: Synthesis and Biological Evaluation. Molecules 2016, 21, 530.

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