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

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

Lijun Wang, Shuaiyu Wang, Bo Jiang, Ning Wu, Xiangqian Li, Baocheng Wang, Jiao Luo, Meng Yang, Shui-Hua Jin, Dayong Shi

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 (4g–4i, 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.

2015

bromophenol, indolin-2-one, anticancer, molecular hybrid, structure–activity relationship

DOI: 10.3390/md13020806

Marine Drugs

MDPI AG

Biology (General)

EN