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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.

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).

SUBMITTER: Fruit C 

PROVIDER: S-EPMC6958357 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature

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

Fruit Corinne C   Couly Florence F   Bhansali Rahul R   Rammohan Malini M   Lindberg Mattias F MF   Crispino John D JD   Meijer Laurent L   Besson Thierry T  

Pharmaceuticals (Basel, Switzerland) 20191217 4

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-<i>f</i>]quinazolin-9(8<i>H</i>)-one (also called <b>FC162</b>) was found to be a promising inhibitor of DYRK1A and was characterized in biological experiments, by western tran  ...[more]

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