Identification of 4-Anilinoquin(az)oline as a Cell-Active Protein Kinase Novel 3 (PKN3) Inhibitor Chemotype

Autor:	Christopher R. M. Asquith, Louisa Temme, Michael P. East, Tuomo Laitinen, Julie Pickett, Frank E. Kwarcinski, Parvathi Sinha, Carrow I. Wells, Gary L. Johnson, Reena Zutshi, David H. Drewry
Rok vydání:	2022
Předmět:	Pharmacology Male Organic Chemistry Drug Discovery Molecular Medicine Humans Prostatic Neoplasms General Pharmacology Toxicology and Pharmaceutics Biochemistry Protein Kinase Inhibitors Protein Kinase C Article
Zdroj:	ChemMedChem
ISSN:	1860-7187
Popis:	Deep annotation of a library of 4-anilinoquinolines led to the identification of 7-iodo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine 16 as a potent inhibitor (IC(50) = 14 nM) of Protein Kinase Novel 3 (PKN3) with micromolar activity in cells. Compound 16 is a potential tool compound to study the cell biology of PKN3 and its role in pancreatic and prostate cancer and T-cell acute lymphoblastic leukemia. These 4-anilinoquinolines may also be useful tools to uncover the therapeutic potential of PKN3 inhibition in a broad range of diseases.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::726b88b789476418a97cda78a2b22181 https://pubmed.ncbi.nlm.nih.gov/35403825 Zobrazit plný text záznamu Plný text