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Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A

Year: 2019
Type: article
Abstract: Dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) hyperactivity has been linked to the development of a number of human malignancies. DYRK1A is the most studied family member, and the discovery of novel specific inhibitors is attracting considerable interest. The 8-cyclopropyl-2(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one (also called FC162) was found to be a promising inhibitor of DYRK1A and was characterized in biological experiments, by western transfer and flow cytometry on SH-SY5Y and pre-B cells. Here, the results obtained with FC162 are compared to well-characterized known DYRK1A inhibitors (e.g., Leucettine L41 and EHT1610).
DOI: 10.3390/ph12040185
Authors: Corinne Fruit, Florence Couly, Rahul Bhansali, Malini Rammohan, Mattias F. Lindberg, John D. Crispino, Laurent Meijer, Thierry Besson
Institutions: Centre National de la Recherche Scientifique, Laboratoire COBRA, Institut National des Sciences Appliquées Rouen Normandie, Northwestern University, University of Illinois Chicago, ManRos Therapeutics (France)
Language: English
Field: Chemistry
Open Access status: gold
Estimated APC paid: $1,013
OpenAlex ID: W2995963445
FWCI: 0.934
Cites: 48
Cited by: 11
Related to: 10