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

Zhao, Shui-Lian; Zhou, Peng; Zhen, Xing-Hua; Han, Yan; Jiang, Haiying; Qu, Youle; Guan, Liping

doi:10.2174/1570180812666141219003209

Cited by 2 publications

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“…In our previous work, we found that compound I [2-(6-bromo-2,3-dioxoindolin-1-yl)-N-(2-bromophenyl) acetamide] displayed inhibitory activity against CDC25B and PTP1B (IC 50 = 3.87 and 2.98 µmol/L, respectively), and also showed cytotoxic activity against three cancer cell lines (HeLa, A549, and HCT116). In addition, compound I displayed potent tumor inhibitory activity in a colo205 xenograft model in vivo (Zhao et al, 2015a). To further investigate the anticancer effects of CDC25B and PTP1B inhibitors, we synthesized a series of 2,3-dioxoindolin-N-phenylacetamide derivatives and investigated the structure-activity relationships.…”

Section: Introductionmentioning

confidence: 99%

Biological evaluation of 2,3-dioxoindolin-N-phenylacetamide derivatives as potent CDC25B and PTP1B phosphatase inhibitors

Jin

Chen

Xia

et al. 2020

Braz. J. Pharm. Sci.

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A series of 2,3-dioxoindolin-N-phenylacetamide derivatives was evaluated for inhibitory activity against CDC25B and PTP1B enzymes. Most of the derivatives showed inhibitory activity against CDC25B (IC 50 = 3.2-23.2 µg/mL) and PTP1B (IC 50 = 2.9-21.4 µg/mL). Compound 2h showed the most inhibitory activity in vitro with IC 50 values of 3.2 and 2.9 µg/mL against CDC25B and PTP1B, respectively, compared with the reference drugs Na 3 VO 4 (IC 50 = 2.7 µg/mL) and oleanolic acid (IC 50 = 2.3 µg/mL). The results of selectivity experiments showed that the 2,3-dioxoindolin-N-phenylacetamide derivatives were selective inhibitors against CDC25B and PTP1B. Enzyme kinetic experiments demonstrated that compound 2h was a specific inhibitor with the typical characteristics of a mixed inhibitor. In cytotoxic activity assays compound 2h had potent activity against A549, HeLa, and HCT116 cell lines. In addition, compound 2h showed potent tumor inhibitory activity in a colo205 xenograft model in vivo.

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Section: Introductionmentioning

confidence: 99%

Biological evaluation of 2,3-dioxoindolin-N-phenylacetamide derivatives as potent CDC25B and PTP1B phosphatase inhibitors

Jin

Chen

Xia

et al. 2020

Braz. J. Pharm. Sci.

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Recent Advances in Research on Active Compounds Against Hepatic Fibrosis

Jin

Liu

et al. 2024

CMC

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Background: Almost all chronic liver diseases cause fibrosis, which can lead to cirrhosis and eventually liver cancer. Liver fibrosis is now considered to be a reversible pathophysiological process and suppression of fibrosis is necessary to prevent liver cancer. At present, no specific drugs have been found that have hepatic anti-fibrotic activity. Objective: The research progress of anti-hepatic fibrosis compounds in recent ten years was reviewed to provide a reference for the design and development of anti-hepatic fibrosis drugs. Methods: According to the structure of the compounds, they are divided into monocyclic compounds, fused-heterocyclic compounds, and acyclic compounds. Results: In this article, the natural products and synthetic compounds with anti-fibrotic activity in recent ten years were reviewed, with emphasis on their pharmacological activity and structure-activity relationship (SAR). Conclusion: Most of these compounds are natural active products and their derivatives, and there are few researches on synthetic compounds and SAR studies on natural product.

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

Cited by 2 publications

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Biological evaluation of 2,3-dioxoindolin-N-phenylacetamide derivatives as potent CDC25B and PTP1B phosphatase inhibitors

Biological evaluation of 2,3-dioxoindolin-N-phenylacetamide derivatives as potent CDC25B and PTP1B phosphatase inhibitors

Recent Advances in Research on Active Compounds Against Hepatic Fibrosis

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