Category: 137837-55-9

Zhang, Shiyan published the artcileDiscovery of a 2-pyridinyl urea-containing compound YD57 as a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1), Category: pyrazoles-derivatives, the publication is European Journal of Medicinal Chemistry (2020), 112277, database is CAplus and MEDLINE.

Inhibition of MAP3K kinase ASK1 has been an attractive strategy for the treatment of nonalcoholic steatohepatitis and multiple sclerosis, among others. Herein, we reported the discovery of 2-pyridinyl urea-containing compound 14l (YD57) as a potent, small-mol. inhibitor of ASK1. 14l was selective against MAP3K kinases ASK2 and TAK1 (>140-fold), while it also inhibited several cell cycle regulating kinases with IC₅₀ values in a range of 90-400 nM (<20-fold selectivity). As a consequence, 14l had stronger apoptosis induction, more potent G1 cell cycle arrest activities, and lower IC₅₀ value of cell growth inhibition than that of GS4997 in HepG2 cancer cell line. On the other hand, 14l did not inhibit ASK1 and p38 phosphorylation in intact cells. We reason that the multi-target effects of 14l likely neutralized the activities caused by inhibition of cellular ASK1. Future studies of these ASK1 inhibitors should pay close attention to their kinome selectivity profile.

European Journal of Medicinal Chemistry published new progress about 137837-55-9. 137837-55-9 belongs to pyrazoles-derivatives, auxiliary class Other Aromatic Heterocyclic,Amine, name is Pyrazolo[1,5-a]pyridin-3-amine, and the molecular formula is C65H82N2O18S2, Category: pyrazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Larsen, Matthew A. published the artcileA Modular and Diastereoselective 5 + 1 Cyclization Approach to N-(Hetero)Aryl Piperidines, Computed Properties of 137837-55-9, the publication is Journal of the American Chemical Society (2020), 142(2), 726-732, database is CAplus and MEDLINE.

A new general de novo synthesis of pharmaceutically important N-(hetero)aryl piperidines is reported. This protocol uses a robustly diastereoselective reductive amination/aza-Michael reaction sequence to achieve rapid construction of complex polysubstituted ring systems starting from widely available heterocyclic amine nucleophiles and carbonyl electrophiles. Notably, the diastereoselectivity of this process is enhanced by the presence of water, and DFT calculations support a stereochem. model involving a facially selective protonation of a water-coordinated enol intermediate.

Journal of the American Chemical Society published new progress about 137837-55-9. 137837-55-9 belongs to pyrazoles-derivatives, auxiliary class Other Aromatic Heterocyclic,Amine, name is Pyrazolo[1,5-a]pyridin-3-amine, and the molecular formula is C7H7N3, Computed Properties of 137837-55-9.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics