Recent advances in the design, synthesis, and biological evaluation of selective DYRK1A inhibitors: a new avenue for a disease modifying treatment of Alzheimer's?

B Smith, F Medda, V Gokhale… - ACS chemical …, 2012 - ACS Publications
DYRK1A inhibitors, for which the majority of efforts have evolved over the last 5 years. In
this review, … inhibitors, and promiscuous kinase inhibitors subsequently found to possess …

New pyrido [3, 4-g] quinazoline derivatives as CLK1 and DYRK1A inhibitors: synthesis, biological evaluation and binding mode analysis

H Tazarki, W Zeinyeh, YJ Esvan, S Knapp… - European Journal of …, 2019 - Elsevier
… CDK5, CK1, GSK3, CLK1 and DYRK1A. Introduction of aminoalkylamino groups at the 2-…
nanomolar affinity and selective inhibition of CLK1 and/or DYRK1A. Their evaluation on several …

DYRK1A inhibitors for disease therapy: Current status and perspectives

T Liu, Y Wang, J Wang, C Ren, H Chen… - European journal of …, 2022 - Elsevier
… In this review, the latest therapeutic potential of DYRK1A for different diseases and the …
This review aims to summarize the recent findings on DYRK1A inhibitors with potential …

Binding mechanism and biological effects of flavone DYRK1A inhibitors for the design of new antidiabetics

K Pustelny, P Grygier, A Barzowska, B Pucelik… - Scientific reports, 2023 - nature.com
… , we decided to verify whether DYRK1A kinase is a molecular … inhibition of DYRK1A by
flavones in biochemical assays. Our X-ray structures confirms flavones interaction with DYRK1A

Discovery of a novel DYRK1A inhibitor with neuroprotective activity by virtual screening and in vitro biological evaluation

X Si, C Qian, N Qiu, Y Wang, M Yao, H Wang… - Molecular Diversity, 2024 - Springer
… to identify novel DYRK1A inhibitors. In this study, we aim to identify structurally diverse
DYRK1A inhibitors for neurodegenerative diseases by VS and in vitro biological evaluation. As …

Selectivity profiling and biological activity of novel β-carbolines as potent and selective DYRK1 kinase inhibitors

K Rüben, A Wurzlbauer, A Walte, W Sippl, F Bracher… - PloS one, 2015 - journals.plos.org
… To evaluate the usability of the new DYRK1A inhibitors in cell culture experiments, we
analyzed the effect of AnnH75 and other harmine analogues on the viability of three different …

Design Synthesis and Biological Evaluation of DYRK1A Inhibitors

Q Zhou - 2017 - ses.library.usyd.edu.au
DYRK1A inhibitors. The work in this thesis explores the importance of the 7-azaindole
skeleton to DYRK1A inhibition … The sequential selectivity of promising inhibitors over other off-…

Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitors: A survey of recent patent literature

TL Nguyen, C Fruit, Y Hérault, L Meijer… - Expert opinion on …, 2017 - Taylor & Francis
… An array of pyrido[3,2-d]pyrimidines was prepared and claimed to inhibit DYRK1A. The patent
assigned to CNRS [Citation39] describes mainly the synthesis and biological evaluation of …

Computational & experimental evaluation of the structure/activity relationship of β-carbolines as DYRK1A inhibitors

B Drung, C Scholz, VA Barbosa, A Nazari… - Bioorganic & medicinal …, 2014 - Elsevier
… Furthermore we validated our theoretical model by synthesis and biological evaluation of
several potential DYRK1A inhibitors. The developed pharmacophore model is able to …

DYRK1A kinase inhibitors with emphasis on cancer

A Ionescu, F Dufrasne, M Gelbcke… - Mini reviews in …, 2012 - ingentaconnect.com
… The current review focuses on the implications of DYRK1A in cancer development, … is
paid to compounds that display anticancer activity through the targeting of DYRK1A. …