Development of a series of novel o-phenylenediamine-based indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors

Autor:	M. Jure-Kunkel, Jay A. Markwalder, Weifang Shan, Bin Chen, Steven P. Seitz, Andrew Nation, John T. Hunt, Lauren Haque, Gregory D. Vite, Jennifer Donnell, David K. Williams, Kelly L. Covello, Aaron Balog, Hart Amy C, Sunil Kumar Mandal, Libing Chen
Rok vydání:	2018
Předmět:	0301 basic medicine Clinical Biochemistry Pharmaceutical Science Phenylenediamines Biochemistry HeLa Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Immune system o-Phenylenediamine Drug Discovery Humans Indoleamine-Pyrrole 2 3 -Dioxygenase Potency Enzyme Inhibitors Indoleamine 2 3-dioxygenase Molecular Biology chemistry.chemical_classification Tumor microenvironment biology Organic Chemistry biology.organism_classification 030104 developmental biology Enzyme chemistry 030220 oncology & carcinogenesis Microsomes Liver Cancer research Molecular Medicine Kynurenine HeLa Cells
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 28:732-736
ISSN:	0960-894X
Popis:	A novel series of o-phenylenediamine-based inhibitors of indoleamine 2,3-dioxygenase (IDO) has been identified. IDO is a heme-containing enzyme, overexpressed in the tumor microenvironment of many cancers, which can contribute to the suppression of the host immune system. Synthetic modifications to a previously described diarylether series resulted in an additional degree of molecular diversity which was exploited to afford compounds that demonstrated significant potency in the HeLa human cervical cancer IDO1 assay. .
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2bfe04a99487884193ada10912d2f182 https://doi.org/10.1016/j.bmcl.2018.01.010 Zobrazit plný text záznamu Full Text from ScienceDirect