6-Bromo-2,3-Dioxoindolin Phenylacetamide Derivatives: Synthesis, Potent CDC25B, PTP1B Inhibitors and Anticancer Activity

Author(s): Shui-Lian Zhao, Zhou Peng, Xing-Hua Zhen, Yan Han, Hai-Ying Jiang, You-Le Qu, Li-Ping Guan

Journal Name: Letters in Drug Design & Discovery

Volume 12 , Issue 7 , 2015

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Graphical Abstract:


A series of 6-bromo-2,3-dioxoindolin phenylacetamide derivatives was synthesized and evaluated for inhibitory activity against CDC25B and PTP1B. Most of the synthesized compounds showed potential inhibitory activities for CDC25B and PTP1B with compound 12 being the most potent (IC50=3.87 µmol/L and 2.98 µmol/L, respectively). Compound 12 also exhibited higher cytotoxic activity against three cancer cell lines (HeLa, A549 and HCT116). In addition, compound 12 delayed the potent tumor inhibitory activity in a colo205 xenograft model in vivo.

Keywords: 2, 3-Dioxoindolin phenylacetamide, CDC25B, PTP1B, MTT, Phosphatase inhibitors, Anticancer activity.

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Article Details

Year: 2015
Published on: 18 December, 2014
Page: [529 - 536]
Pages: 8
DOI: 10.2174/1570180812666141219003209
Price: $65

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