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Mar. Drugs 2017, 15(11), 343; doi:10.3390/md15110343

Discovery of Novel Bromophenol Hybrids as Potential Anticancer Agents through the Ros-Mediated Apoptotic Pathway: Design, Synthesis and Biological Evaluation

Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, Shandong, China
Laboratory for Marine Drugs and Bioproducts, Qingdao National Laboratory for Marine Science and Technology, Qingdao 266071, Shandong, China
University of Chinese Academy of Sciences, Beijing 10049, China
These authors contributed equally to this work.
Author to whom correspondence should be addressed.
Received: 23 September 2017 / Revised: 18 October 2017 / Accepted: 30 October 2017 / Published: 1 November 2017
(This article belongs to the Special Issue Synthesis of Marine-Derived Compounds)
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A series of bromophenol hybrids with N-containing heterocyclic moieties were designed, and their anticancer activities against a panel of five human cancer cell lines (A549, Bel7402, HepG2, HCT116 and Caco2) using MTT assay in vitro were explored. Among them, thirteen compounds (17a, 17b, 18a, 19a, 19b, 20a, 20b, 21a, 21b, 22a, 22b, 23a, and 23b) exhibited significant inhibitory activity against the tested cancer cell lines. The structure-activity relationships (SARs) of bromophenol derivatives were discussed. The promising candidate compound 17a could induce cell cycle arrest at G0/G1 phase and induce apoptosis in A549 cells, as well as caused DNA fragmentations, morphological changes and ROS generation by the mechanism studies. Furthermore, compound 17a suppression of Bcl-2 levels (decrease in the expression of the anti-apoptotic proteins Bcl-2 and down-regulation in the expression levels of Bcl-2) in A549 cells were observed, along with activation caspase-3 and PARP, which indicated that compound 17a induced A549 cells apoptosis in vitro through the ROS-mediated apoptotic pathway. These results might be useful for bromophenol derivatives to be explored and developed as novel anticancer drugs. View Full-Text
Keywords: bromophenol hybrids; anticancer; structure-activity relationships; ROS; apoptotic pathway bromophenol hybrids; anticancer; structure-activity relationships; ROS; apoptotic pathway

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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Wang, L.-J.; Guo, C.-L.; Li, X.-Q.; Wang, S.-Y.; Jiang, B.; Zhao, Y.; Luo, J.; Xu, K.; Liu, H.; Guo, S.-J.; Wu, N.; Shi, D.-Y. Discovery of Novel Bromophenol Hybrids as Potential Anticancer Agents through the Ros-Mediated Apoptotic Pathway: Design, Synthesis and Biological Evaluation. Mar. Drugs 2017, 15, 343.

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