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Biological evaluation of 2,3-dioxoindolin-N-phenylacetamide derivatives as potent CDC25B and PTP1B phosphatase inhibitors
Jin, Qing-Hao; Chen, Wen-Bo; Xia, Ya-Nan; Liu, Bing-Yu; Guan, Li-Ping.
  • Jin, Qing-Hao; Zhejiang Ocean University. DongHai Science and Technology College. Zhejiang. CN
  • Chen, Wen-Bo; Zhejiang Ocean University. DongHai Science and Technology College. Zhejiang. CN
  • Xia, Ya-Nan; Zhejiang Ocean University. Food and Pharmacy College. Zhejiang. CN
  • Liu, Bing-Yu; Zhejiang Ocean University. Food and Pharmacy College. Zhejiang. CN
  • Guan, Li-Ping; Zhejiang Ocean University. Food and Pharmacy College. Zhejiang. CN
Braz. J. Pharm. Sci. (Online) ; 56: e00222, 2020. tab, graf
Article in English | LILACS-Express | LILACS | ID: biblio-1089183
ABSTRACT
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 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.


Full text: Available Index: LILACS (Americas) Type of study: Prognostic study Language: English Journal: Braz. J. Pharm. Sci. (Online) Journal subject: Farmacologia / Terapˆutica / Toxicologia Year: 2020 Type: Article / Project document Affiliation country: China Institution/Affiliation country: Zhejiang Ocean University/CN

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Full text: Available Index: LILACS (Americas) Type of study: Prognostic study Language: English Journal: Braz. J. Pharm. Sci. (Online) Journal subject: Farmacologia / Terapˆutica / Toxicologia Year: 2020 Type: Article / Project document Affiliation country: China Institution/Affiliation country: Zhejiang Ocean University/CN