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