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Provedor de dados:  BJPS
País:  Brazil
Título:  Biological evaluation of 2,3-dioxoindolin-N-phenylacetamide derivatives as potent CDC25B and PTP1B phosphatase inhibitors
Autores:  Jin,Qing-Hao
Chen,Wen-Bo
Xia,Ya-Nan
Liu,Bing-Yu
Guan,Li-Ping
Data:  2020-01-01
Ano:  2020
Palavras-chave:  Dioxoindolin-N-phenylacetamide
CDC25B
PTP1B
Phosphatase inhibitors
Enzyme kinetics
Resumo:  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.
Tipo:  Info:eu-repo/semantics/article
Idioma:  Inglês
Identificador:  http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100500
Editor:  Universidade de São Paulo, Faculdade de Ciências Farmacêuticas
Relação:  10.1590/s2175-97902019000400222
Formato:  text/html
Fonte:  Brazilian Journal of Pharmaceutical Sciences v.56 2020
Direitos:  info:eu-repo/semantics/openAccess
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