Potent CDC25B and PTP1B phosphatase inhibitors: 2′,4′,6′-trihydroxylchalcone derivatives.

In this study, we examined a series of 2′,4′,6′-trihydroxychalcone derivatives for their inhibitory activity as inhibitors of CDC25B and PTP1B. The pharmacological results showed that all of the tested compounds significantly inhibited CDC25B and PTP1B phosphatase in vitro. Among them, three compounds 2, 6, and 7 had the best inhibition activity, with inhibition rates against CDC25B were 99.56, 99.68, and 99.63 %, respectively, and with inhibition rates against PTP1B were 98.99, 99.37, and 98.08 %, respectively, which is similar to reference drugs NaVO and Oleanolic acid, respectively. Cytotoxic activity assays showed compounds 2, 6, and 7 are potent against HeLa and HCT116. Moreover, compound 6 delayed the potent antitumor inhibitory activity in a colo205 xenograft model in vivo. [ABSTRACT FROM AUTHOR]