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新型含吲哚啉-2-酮部分的溴酚衍生物作为潜在抗癌剂的设计、合成及生物学评价

Design, synthesis and biological evaluation of novel bromophenol derivatives incorporating indolin-2-one moiety as potential anticancer agents.

作者信息

Wang Li-Jun, Wang Shuai-Yu, Jiang Bo, Wu Ning, Li Xiang-Qian, Wang Bao-Cheng, Luo Jiao, Yang Meng, Jin Shui-Hua, Shi Da-Yong

机构信息

Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China.

出版信息

Mar Drugs. 2015 Feb 2;13(2):806-23. doi: 10.3390/md13020806.

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 (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.

摘要

设计并评估了一系列含有吲哚啉-2-酮部分的溴酚衍生物,通过体外MTT试验检测它们对A549、Bel7402、HepG2、HeLa和HCT116癌细胞系的抗癌活性。其中,七种化合物(4g-4i、5h、6d、7a、7b)对所测试的五种人类癌细胞系显示出强效活性。伤口愈合试验表明,化合物4g可作为一种强效化合物,通过抑制癌细胞迁移来使侵袭和转移失活。讨论了溴酚衍生物的构效关系(SARs),这对于探索和开发溴酚衍生物作为新型抗癌药物很有用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36ee/4344603/56124e31fa73/marinedrugs-13-00806-g001.jpg

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