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

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

Volume: 12 Issue: 7

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

Affiliation:

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

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.

Cite this article as:

Zhao Shui-Lian, Peng Zhou, Zhen Xing-Hua, Han Yan, Jiang Hai-Ying, Qu You-Le and Guan Li-Ping, 6-Bromo-2,3-Dioxoindolin Phenylacetamide Derivatives: Synthesis, Potent CDC25B, PTP1B Inhibitors and Anticancer Activity, Letters in Drug Design & Discovery 2015; 12 (7) . https://dx.doi.org/10.2174/1570180812666141219003209