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Pharmaceuticals
Volume 12
Issue 4
10.3390/ph12040185
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Open AccessCommunication

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,*
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)
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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). View Full-Text
Keywords: thiazolo[5,4-f]quinazolin-9(8H)-one; CMGC kinases; DYRK family kinases; SH-SY5Y-Tau-4R cells; pre-B cells; quiescence 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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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited

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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. https://doi.org/10.3390/ph12040185

AMA Style

Fruit C, Couly F, Bhansali R, Rammohan M, Lindberg MF, Crispino JD, 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(4):185. https://doi.org/10.3390/ph12040185

Chicago/Turabian Style

Fruit, Corinne; Couly, Florence; Bhansali, Rahul; Rammohan, Malini; Lindberg, Mattias F.; Crispino, John D.; Meijer, Laurent; Besson, Thierry. 2019. "Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A" Pharmaceuticals 12, no. 4: 185. https://doi.org/10.3390/ph12040185

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