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Mar. Drugs 2015, 13(2), 806-823; doi:10.3390/md13020806

Design, Synthesis and Biological Evaluation of Novel Bromophenol Derivatives Incorporating Indolin-2-One Moiety as Potential Anticancer Agents

Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China
These authors contributed equally to this work.
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Author to whom correspondence should be addressed.
Academic Editor: Yoshihide Usami
Received: 31 December 2014 / Accepted: 27 January 2015 / Published: 2 February 2015
(This article belongs to the Special Issue Synthesis around Marine Natural Products)
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Abstract

A series of bromophenol derivatives containing indolin-2-one moiety were designed and evaluated that for their anticancer activities against A549, Bel7402, HepG2, HeLa and HCT116 cancer cell lines using MTT assay in vitro. Among them, seven compounds (4g4i, 5h, 6d, 7a, 7b) showed potent activity against the tested five human cancer cell lines. Wound-healing assay demonstrated that compound 4g can be used as a potent compound for inactivating invasion and metastasis by inhibiting the migration of cancer cells. The structure–activity relationships (SARs) of bromophenol derivatives had been discussed, which were useful for exploring and developing bromophenol derivatives as novel anticancer drugs. View Full-Text
Keywords: bromophenol; indolin-2-one; anticancer; molecular hybrid; structure–activity relationship bromophenol; indolin-2-one; anticancer; molecular hybrid; structure–activity relationship
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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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MDPI and ACS Style

Wang, L.-J.; Wang, S.-Y.; Jiang, B.; Wu, N.; Li, X.-Q.; Wang, B.-C.; Luo, J.; Yang, M.; Jin, S.-H.; Shi, D.-Y. Design, Synthesis and Biological Evaluation of Novel Bromophenol Derivatives Incorporating Indolin-2-One Moiety as Potential Anticancer Agents. Mar. Drugs 2015, 13, 806-823.

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