Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A
by
Corinne Fruit 1
, Florence Couly 1, Rahul Bhansali 2,3, Malini Rammohan 2, Mattias F. Lindberg 4, John D. Crispino 2,5, Laurent Meijer 4 and Thierry Besson 1,*
Corinne Fruit 1, Florence Couly 1, Rahul Bhansali 2,3, Malini Rammohan 2, Mattias F. Lindberg 4, John D. Crispino 2,5, Laurent Meijer 4 and Thierry Besson 1,*
1
Normandie Univ, UNIROUEN, INSA Rouen, CNRS, COBRA UMR 6014, 76000 Rouen, France
2
Department of Medicine, Division of Hematology/Oncology, Northwestern University, Chicago, IL 60611, USA
3
College of Medicine, University of Illinois, Chicago, IL 60611, USA
4
ManRos Therapeutics & Perha Pharmaceuticals, Perharidy Peninsula, 29680 Roscoff, France
5
Department of Biochemistry and Molecular Genetics, Northwestern University Feinberg School of Medicine, Chicago, IL 60611, USA
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2019, 12(4), 185; https://doi.org/10.3390/ph12040185
Received: 18 October 2019 / Revised: 13 December 2019 / Accepted: 14 December 2019 / Published: 17 December 2019
(This article belongs to the Special Issue Recent Contributions in Medicinal Chemistry Within European GP2A Network)
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).
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Keywords:
thiazolo[5,4-f]quinazolin-9(8H)-one; CMGC kinases; DYRK family kinases; SH-SY5Y-Tau-4R cells; pre-B cells; quiescence
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MDPI and ACS Style
Fruit, C.; Couly, F.; Bhansali, R.; Rammohan, M.; Lindberg, M.F.; Crispino, J.D.; Meijer, L.; Besson, T. Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A. Pharmaceuticals 2019, 12, 185.
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