Advances in the discovery of selective JAK inhibitors

CJ Menet, L Van Rompaey, R Geney - Progress in medicinal chemistry, 2013 - Elsevier
In this review, we describe the current knowledge of the biology of the JAKs. The JAK family
comprises the four nonreceptor tyrosine kinases JAK1, JAK2, JAK3, and Tyk2, all key …

The use of conformational restriction in medicinal chemistry

P de Sena M Pinheiro, DA Rodrigues… - Current topics in …, 2019 - ingentaconnect.com
During the early preclinical phase, from hit identification and optimization to a lead
compound, several medicinal chemistry strategies can be used to improve potency and/or …

[HTML][HTML] Apigenin ameliorates hyperuricemia and renal injury through regulation of uric acid metabolism and JAK2/STAT3 signaling pathway

T Liu, H Gao, Y Zhang, S Wang, M Lu, X Dai, Y Liu… - Pharmaceuticals, 2022 - mdpi.com
Hyperuricemia (HUA) is a kind of metabolic disease with high incidence that still needs new
countermeasures. Apigenin has uric-lowering and kidney-protective activities, but how …

Vibrational (FT-IR and FT-Raman), electronic (UV–Vis), NMR (1H and 13C) spectra and molecular docking analyses of anticancer molecule 4-hydroxy-3 …

K Thirunavukkarasu, P Rajkumar, S Selvaraj… - Journal of Molecular …, 2018 - Elsevier
Abstract The structure of 4-Hydroxy-3-methoxycinnamaldehyde (4H3MC) has been
analyzed by spectroscopic and theoretical investigations. The vibrational spectral analysis of …

Cytotoxicity, in silico predictions and molecular studies for androstane heterocycle compounds revealed potential antitumor agent against lung cancer cells

MA Tantawy, S Shaheen, SW Kattan… - Journal of …, 2022 - Taylor & Francis
Abstract The IL6/JAK2/STAT3 axis dysregulation and the related downstream pathways are
a major contributor to the progression of non-small-cell lung carcinoma (NSCLC) and mainly …

[HTML][HTML] Research and progress on ClC‑2

H Wang, M Xu, Q Kong, P Sun… - Molecular …, 2017 - spandidos-publications.com
Abstract Chloride channel 2 (ClC-2) is one of the nine mammalian members of the ClC
family. The present review discusses the molecular properties of ClC‑2, including CLCN2 …

Development and a practical synthesis of the JAK2 inhibitor LY2784544

D Mitchell, KP Cole, PM Pollock… - … Process Research & …, 2012 - ACS Publications
The route selection and process research and development of a practical synthesis for JAK2
inhibitor LY2784544 is described. The first-generation synthesis route, similar to that used in …

Discovery of JAK2/3 inhibitors from quinoxalinone-containing compounds

K Sanachai, P Mahalapbutr, L Tabtimmai… - ACS …, 2022 - ACS Publications
Janus kinases (JAKs) are involved in a wide variety of cell signaling associated with T-cell
and B-cell mediated diseases. The pathogenesis of common lymphoid-derived diseases …

[HTML][HTML] Upregulation of peptide transporters PEPT1 and PEPT2 by Janus kinase JAK2

Z Hosseinzadeh, L Dong, SK Bhavsar, J Warsi… - Cellular Physiology and …, 2013 - karger.com
Background/Aims: Janus-activated kinase-2 JAK2 participates in the signaling of several
hormones including growth hormone, fosters tumor growth and modifies the activity of …

Novel pyrrole carboxamide inhibitors of JAK2 as potential treatment of myeloproliferative disorders

MG Brasca, P Gnocchi, M Nesi, N Amboldi… - Bioorganic & Medicinal …, 2015 - Elsevier
Compound 1, a hit from the screening of our chemical collection displaying activity against
JAK2, was deconstructed for SAR analysis into three regions, which were explored. A series …