Discovery of in vivo active sphingosine-1-phosphate transporter (Spns2) inhibitors

R Fritzemeier, D Foster, A Peralta… - Journal of medicinal …, 2022 - ACS Publications
Sphingosine 1-phosphate (S1P) is a pleiotropic signaling molecule that interacts with five G-
protein-coupled receptors (S1P1-5) to regulate cellular signaling pathways. S1P export is …

Discovery and biological evaluation of biaryl acetamide derivatives as selective and in vivo active sphingosine kinase-2 inhibitors

Y Li, G Li, Y Wang, L Li, Y Song, F Cao… - European Journal of …, 2024 - Elsevier
Abstract Sphingosine kinase 2 (SphK2) has emerged as a promising target for cancer
therapy due to its critical role in tumor growth. However, the lack of potent and selective …

A Novel Sphingosine Kinase Inhibitor Suppresses Chikungunya Virus Infection

OO Oyewole, K Dunnavant, S Bhattarai, Y Kharel… - Viruses, 2022 - mdpi.com
Chikungunya virus (CHIKV) is a re-emerging arbovirus in the alphavirus genus. Upon
infection, it can cause severe joint pain that can last years in some patients, significantly …

Indole and indoline scaffolds in drug discovery

F Liu, M Su - Privileged Scaffolds in Drug Discovery, 2023 - Elsevier
As privileged scaffolds and versatile pharmacophores, indole and indoline demonstrate an
array of biological activities relevant to numerous human diseases and are present in many …

[PDF][PDF] Synthesis, Characterisation and Binding Evaluation of New 6-Amidinoindole Compound as the Potential Heme Binder

NAK JILANI, N OKA, K ANDO, SA HASBULLAH - Sains Malaysiana, 2023 - ukm.edu.my
In this study, the new compound 6-amidinoindole 3 were synthesized by hydrogenating the
amidoxime unit in a high yield. The compound was characterized by FTIR, 1H NMR, 13C …

[HTML][HTML] Revealing 2-dimethylhydrazino-2-alkyl alkynyl sphingosine derivatives as sphingosine kinase 2 inhibitors: Some hints on the structural basis for selective …

M Corro-Moron, A Granell, V Ivanova, E Domingo… - Bioorganic …, 2022 - Elsevier
Sphingosine kinase (SphK), which catalyzes the transfer of phosphate from ATP to
sphingosine (Sph) generating sphingosine-1-phosphate (S1P) has emerged as therapeutic …

Development of Potent Inhibitors of the Sphingosine-1-Phosphate Transporter Spns2 for the Treatment of Multiple Sclerosis

DJ Foster - 2022 - vtechworks.lib.vt.edu
Abstract Sphingosine-1-phosphate (S1P) is an amino-alcohol signaling molecule produced
from the intracellular phosphorylation of the lipid sphingosine. Despite possessing several …

[PDF][PDF] Development of Novel Methods for the Installation of Trifluoromethyl/Boryl and 1, 2, 4–Oxadiazole Moieties

S Jos - 2022 - vtechworks.lib.vt.edu
There are immense efforts to install the trifluoromethyl group (CF3) into organic molecules
since it significantly affects reactivity, as well as the biological and pharmaceutical properties …