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

Pub. Date : 2018 Sep 5

PMID : 30193214






1 Functional Relationships(s)
Download
Sentence
Compound Name
Protein Name
Organism
1 Herein, we describe the design and synthesis of a series of amide functionalized 2,4-bispyridyl thiophene compounds, of which the 4-fluorobenzyl amide derivative (31b) displayed the highest potency against Dyrk1A and remarkable selectivity over closely related kinases (IC50: Dyrk1A = 14.3 nM; Dyrk1B = 383 nM, Clk1 > 2 muM). 4-fluorobenzamide CDC like kinase 1 Homo sapiens