Revue: | Brazilian Journal of Pharmaceutical Sciences |
Base de datos: | PERIÓDICA |
Número de sistema: | 000451491 |
ISSN: | 1984-8250 |
Autores: | Jin, Qing Hao1 Chen, Wen Bo1 Xia, Ya Nan2 Liu, Bing Yu2 Guan, Li Ping2 |
Instituciones: | 1Zhejiang Ocean University, DongHai Science and Technology College, Zhejiang, Zhoushan. China 2Zhejiang Ocean University, Food and Pharmacy College, Zhejiang, Zhoushan. China |
Año: | 2020 |
Volumen: | 56 |
País: | Brasil |
Idioma: | Inglés |
Tipo de documento: | Artículo |
Enfoque: | Experimental, aplicado |
Resumen en inglés | 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 |
Disciplinas: | Química |
Palabras clave: | Química farmacéutica, Bioquímica, Dioxoindolina-N-fenilacetamida, Cinética enzimática, Inhibidores enzimáticos, Fosfatasas |
Keyword: | Medicinal chemistry, Biochemistry, Dioxoindolin-N-phenylacetamide, Enzymatic kinetics, Phosphatases |
Texte intégral: | Texto completo (Ver HTML) Texto completo (Ver PDF) |