[HTML][HTML] [b]-Annulated Halogen-Substituted Indoles as Potential DYRK1A Inhibitors

C Lechner, M Flaßhoff, H Falke, L Preu, N Loaëc… - Molecules, 2019 - mdpi.com
Since hyperactivity of the protein kinase DYRK1A is linked to several neurodegenerative
disorders, DYRK1A inhibitors have been suggested as potential therapeutics for Down …

DYRK1A kinase inhibition with emphasis on neurodegeneration: A comprehensive evolution story-cum-perspective

A Pathak, A Rohilla, T Gupta, MJ Akhtar… - European Journal of …, 2018 - Elsevier
Alzheimer, the fourth leading cause of death embodies a key responsible event including
formation of β-amyloid protein clustering to amyloid plaque on blood vessels. The origin of …

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
With 24.3 million people affected in 2005 and an estimated rise to 42.3 million in 2020,
dementia is currently a leading unmet medical need and costly burden on public health …

Development of novel 2, 4-bispyridyl thiophene–based compounds as highly potent and selective Dyrk1A inhibitors. Part I: benzamide and benzylamide derivatives

SS Darwish, M Abdel-Halim, M Salah, AH Abadi… - European Journal of …, 2018 - Elsevier
The protein kinase Dyrk1A modulates several processes relevant to the development or
progression of Alzheimer's disease (AD), eg through phosphorylation of tau protein, amyloid …

Development of novel amide–derivatized 2, 4-bispyridyl thiophenes as highly potent and selective Dyrk1A inhibitors. Part II: Identification of the cyclopropylamide …

SS Darwish, M Abdel-Halim, AK ElHady… - European Journal of …, 2018 - Elsevier
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (Dyrk1A) is a potential target
in Alzheimer's disease (AD) because of the established correlation between its over …

[HTML][HTML] Indole-3-carbonitriles as DYRK1A inhibitors by fragment-based drug design

R Meine, W Becker, H Falke, L Preu, N Loaëc, L Meijer… - Molecules, 2018 - mdpi.com
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a potential drug
target because of its role in the development of Down syndrome and Alzheimer's disease …

DYRK1A Inhibitors and Perspectives for the Treatment of Alzheimer's Disease

MM de Souza, AR Cenci, KF Teixeira… - Current Medicinal …, 2023 - ingentaconnect.com
Background: Alzheimer's disease (AD) is a chronic neurodegenerative disease and the most
common form of dementia, especially in the elderly. Due to the increase in life expectancy, in …

10-Iodo-11H-indolo[3,2-c]quinoline-6-carboxylic Acids Are Selective Inhibitors of DYRK1A

H Falke, A Chaikuad, A Becker, N Loaëc… - Journal of medicinal …, 2015 - ACS Publications
The protein kinase DYRK1A has been suggested to act as one of the intracellular regulators
contributing to neurological alterations found in individuals with Down syndrome. For an …

DYRK1A inhibition as potential treatment for Alzheimer's disease

S Stotani, F Giordanetto, F Medda - Future medicinal chemistry, 2016 - Taylor & Francis
In total, 47,500,000 people worldwide are affected by dementia and this number is estimated
to double by 2030 and triple within 2050 resulting in a huge burden on public health …

DYRK1A inhibitors for disease therapy: Current status and perspectives

T Liu, Y Wang, J Wang, C Ren, H Chen… - European journal of …, 2022 - Elsevier
Dual-specificity tyrosine phosphorylation-regulated kinase 1 A (DYRK1A) is a conserved
protein kinase that plays essential roles in various biological processes. It is located in the …