949-30-4Relevant academic research and scientific papers
AUTOTAXIN INHIBITORS
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Page/Page column 18; 30; 23; 37, (2018/01/17)
The present disclosure provides novel ATX inhibitors, and pharmaceutical compositions comprising said inhibitors, as well as methods of treatment comprising administration of said inhibitors.
Highly Potent Non-Carboxylic Acid Autotaxin Inhibitors Reduce Melanoma Metastasis and Chemotherapeutic Resistance of Breast Cancer Stem Cells
Banerjee, Souvik,Norman, Derek D.,Lee, Sue Chin,Parrill, Abby L.,Pham, Truc Chi T.,Baker, Daniel L.,Tigyi, Gabor J.,Miller, Duane D.
, p. 1309 - 1324 (2017/03/08)
Autotaxin (ATX, aka. ENPP2) is the main source of the lipid mediator lysophosphatidic acid (LPA) in biological fluids. This study reports on inhibitors of ATX derived by lead optimization of the benzene-sulfonamide in silico hit compound 3. The new analogues provide a comprehensive structure-activity relationship of the benzene-sulfonamide scaffold that yielded a series of highly potent ATX inhibitors. The three most potent analogues (3a, IC50 ～ 32 nM; 3b, IC50 ～ 9 nM; and 14, IC50 ～ 35 nM) inhibit ATX-dependent invasion of A2058 human melanoma cells in vitro. Two of the most potent compounds, 3b and 3f (IC50 ～ 84 nM), lack inhibitory action on ENPP6 and ENPP7 but possess weak antagonist action specific to the LPA1 G protein-coupled receptor. In particular, compound 3b potently reduced in vitro chemotherapeutic resistance of 4T1 breast cancer stem-like cells to paclitaxel and significantly reduced B16 melanoma metastasis in vivo.
Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates
Sun, Lian-Qi,Zhu, Lei,Qian, Keduo,Qin, Bingjie,Huang, Li,Chen, Chin Ho,Lee, Kuo-Hsiung,Xie, Lan
, p. 7219 - 7229 (2012/11/07)
Twenty-one new 4-substituted diarylaniline compounds (DAANs) (series 13, 14, and 15) were designed, synthesized, and evaluated against wildtype and drug resistant HIV-1 viral strains. As a result, approximately a dozen new DAANs showed high potency with l
Use of EP4 receptor ligands in the treatment of IL-6 involved diseases
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Page 119, (2010/02/06)
Methods of treating IL-6 involved diseases with EP4 receptor ligands, including EP4 receptor antagonists. Assays to determine the effect of test compounds on PGE2-induced whole blood cells activation.
EP4 RECEPTOR INHIBITORS TO TREAT RHEUMATOID ARTHRITIS
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, (2008/06/13)
The invention features a method of treating rheumatoid arthritis in a mammal comprising administering an agent that inhibits prostaglandin EP4 receptor (EP4) activity. Also featured is a method of identifying agents that selectively inhibit EP4 activity in vivo.
