Identification of a series of substituted 2-piperazinyl-5-pyrimidylhydroxamic acids as potent histone deacetylase inhibitors

Autor:	Bruno Roux, Luc Van Hijfte, Jacky van Gompel, Claire Mackie, Sven Franciscus Anna Janssen Pharm. Van Brandt, Marc Noppe, Ann Marien, David Speybrouck, Lut Janssen, Marc Du Jardin, Wim Floren, Eddy Jean Edgard Freyne, Michel Janicot, Kristof Van Emelen, Jacky Van Dun, Ron Gilissen, Isabelle Noëlle Constance Pilatte, Virginie Sophie Poncelet, Patrick Angibaud, Verdonck Marc Gustaaf Celine, Peter ten Holte, Sandrine Gaurrand, Martin John Page, Jozef Peeters, Laurence Decrane, Janine Arts, Laurence Queguiner
Rok vydání:	2009
Předmět:	medicine.drug_class Clinical Biochemistry Pharmaceutical Science Mice Nude Antineoplastic Agents Hydroxamic Acids Biochemistry Histone Deacetylases Rats Sprague-Dawley chemistry.chemical_compound Mice Structure-Activity Relationship In vivo Cell Line Tumor Drug Discovery medicine Structure–activity relationship Animals Cytotoxicity Molecular Biology Cell Proliferation chemistry.chemical_classification Hydroxamic acid biology Organic Chemistry Histone deacetylase inhibitor Xenograft Model Antitumor Assays Rats Histone Deacetylase Inhibitors Enzyme chemistry Enzyme inhibitor Drug Design biology.protein Molecular Medicine Histone deacetylase
Zdroj:	Bioorganicmedicinal chemistry letters. 20(1)
ISSN:	1464-3405
Popis:	Pursuing our efforts in designing 5-pyrimidylhydroxamic acid anti-cancer agents, we have identified a new series of potent histone deacetylase (HDAC) inhibitors. These compounds exhibit enzymatic HDAC inhibiting properties with IC(50) values in the nanomolar range and inhibit tumor cell proliferation at similar levels. Good solubility, moderate bioavailability, and promising in vivo activity in xenograft model made this series of compounds interesting starting points to design new potent HDAC inhibitors.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cc639d3fe98001df6eb7f54901be8937 https://pubmed.ncbi.nlm.nih.gov/19906529 Zobrazit plný text záznamu Full Text from ScienceDirect