Balancing Histone Deacetylase (HDAC) Inhibition and Drug‐likeness: Biological and Physicochemical Evaluation of Class I Selective HDAC Inhibitors

Autor:	Linda Schäker‐Hübner, Reza Haschemi, Thomas Büch, Fabian B. Kraft, Birke Brumme, Andrea Schöler, Robert Jenke, Jens Meiler, Achim Aigner, Gerd Bendas, Finn K. Hansen
Rok vydání:	2022
Předmět:	Histone Deacetylase Inhibitors Pharmacology Peptoids Organic Chemistry Drug Discovery Molecular Medicine Histone Deacetylase 1 General Pharmacology Toxicology and Pharmaceutics Biochemistry Histone Deacetylases
Zdroj:	ChemMedChem. 17
ISSN:	1860-7187 1860-7179
DOI:	10.1002/cmdc.202100755
Popis:	Herein we report the structure-activity and structure-physicochemical property relationships of a series of class I selective ortho-aminoanilides targeting the "foot-pocket" in HDAC12. To balance the structural benefits and the physicochemical disadvantages of these substances, we started with a set of HDACi related to tacedinaline (CI-994) and evaluated their solubility, lipophilicity (log D
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::719df0fdda32b3c206d20d07a15eaf64 https://doi.org/10.1002/cmdc.202100755 Zobrazit plný text záznamu Plný text