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Biological evaluation of 2,3-dioxoindolin-N-phenylacetamide derivatives as potent CDC25B and PTP1B phosphatase inhibitors BJPS
Jin,Qing-Hao; Chen,Wen-Bo; Xia,Ya-Nan; Liu,Bing-Yu; Guan,Li-Ping.
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 (IC50 = 3.2-23.2 µg/mL) and PTP1B (IC50 = 2.9-21.4 µg/mL). Compound 2h showed the most inhibitory activity in vitro with IC50 values of 3.2 and 2.9 µg/mL against CDC25B and PTP1B, respectively, compared with the reference drugs Na3VO4 (IC50 = 2.7 µg/mL) and oleanolic acid (IC50 = 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...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Dioxoindolin-N-phenylacetamide; CDC25B; PTP1B; Phosphatase inhibitors; Enzyme kinetics.
Ano: 2020 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100500
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