Design, synthesis and biological evaluation of 4-piperazinyl-containing Chidamide derivatives as HDACs inhibitors

Autor:	Jianqi Li, Qingwei Zhang, Bingliu Lu
Rok vydání:	2017
Předmět:	0301 basic medicine Cell Survival Clinical Biochemistry hERG Transplantation Heterologous Pharmaceutical Science Administration Oral Aminopyridines Antineoplastic Agents Pharmacology Biochemistry Histone Deacetylases Piperazines Rats Sprague-Dawley 03 medical and health sciences chemistry.chemical_compound Mice 0302 clinical medicine In vivo Chidamide Catalytic Domain Cell Line Tumor Drug Discovery Animals Humans Binding site Molecular Biology Ion channel Biological evaluation Binding Sites biology Chemistry Organic Chemistry HCT116 Cells HDAC1 Rats Histone Deacetylase Inhibitors Molecular Docking Simulation 030104 developmental biology 030220 oncology & carcinogenesis Drug Design Toxicity Benzamides Colonic Neoplasms biology.protein Molecular Medicine Female Drug Screening Assays Antitumor Half-Life
Zdroj:	Bioorganicmedicinal chemistry letters. 27(14)
ISSN:	1464-3405
Popis:	The synthesis and biological evaluation of a variety of 4-piperazinyl-containing Chidamide derivatives is described. Some of these compounds were shown to inhibit HDAC1 with IC50 values below micromolar range, and inhibited proliferation of several human cancer cells, not possessing toxicity to human normal cells and hERG K+ ion channels. Compound 9g, proved to be the most potent and efficacious derivative in this series, was orally active in an HCT116 xenograft model in vivo.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2e2e66d05b75f3ee059734d05908a2b https://pubmed.ncbi.nlm.nih.gov/28532668 Zobrazit plný text záznamu Full Text from ScienceDirect