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Discovery of Indole-Piperazine Hybrid Structures as Potent Selective Class I Histone Deacetylases Inhibitors.
Xing, Liang; Gong, Guoliang; Chen, Xinyang; Chen, Xin.
Afiliação
  • Xing L; Guangxi Key Laboratory of Urban Water Environment, College of Chemistry and Environmental Engineering, Baise University.
  • Gong G; Shaanxi Key Labotory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University.
  • Chen X; Shaanxi Key Labotory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University.
  • Chen X; Shaanxi Key Labotory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University.
Chem Pharm Bull (Tokyo) ; 71(3): 206-212, 2023.
Article em En | MEDLINE | ID: mdl-36858525
Histone deacetylases (HDACs) are important targets in cancer treatment, and the development of selective and broad-spectrum HDACs inhibitors (HDACis) is urgent. In this research, a series of aroylpiperazine hybrid derivatives were designed and synthesized. Among these, indole-piperazine hybrids 6a (IC50 = 205 nM) and 6b (IC50 = 280 nM) showed submicromolar activity against HDAC1. Moreover, 6a showed a preferable affinity toward class I HDACs, especially for HDAC1-3. In vitro, 6a exhibited better antiproliferative activities against K562 and HCT116 cell lines than chidamide.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores de Histona Desacetilases / Histona Desacetilases Limite: Humans Idioma: En Revista: Chem Pharm Bull (Tokyo) Ano de publicação: 2023 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores de Histona Desacetilases / Histona Desacetilases Limite: Humans Idioma: En Revista: Chem Pharm Bull (Tokyo) Ano de publicação: 2023 Tipo de documento: Article