Design, Synthesis, and Biological Evaluation of (Hydroxyphenyl)naphthalene and -quinoline Derivatives: Potent and Selective Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1) for the Treatment of Estrogen-Dependent Diseases

2008 ◽  
Vol 51 (7) ◽  
pp. 2158-2169 ◽  
Author(s):  
Martin Frotscher ◽  
Erika Ziegler ◽  
Sandrine Marchais-Oberwinkler ◽  
Patricia Kruchten ◽  
Alexander Neugebauer ◽  
...  
Keyword(s):  
Hydroxysteroid Dehydrogenase ◽  
Biological Evaluation ◽  
Quinoline Derivatives ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation as immunosuppressant of amino alcohol derivatives containing thioether

2021 ◽  
Vol 11 (5) ◽  
pp. 773-780
Author(s):  
Yanjie Li ◽  
Yongqiang Li ◽  
Liu Yang ◽  
Zhi Liu ◽  
Ruimeng Zhang ◽  
...  
Keyword(s):  
Amino Alcohol ◽  
Coupling Reaction ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Suzuki Coupling Reaction ◽  
Sphingosine 1 Phosphate ◽  
Potential Activity ◽  
Key Steps ◽  
Synthesis And Biological Evaluation

To develop a safer immunosuppressant for organ transplantation and autoimmune disease treatment, in this study, several of novel amino alcohol derivatives containing thioether moiety were synthesized with 7-bromo-tetralin-2-one as starting material, and Suzuki coupling reaction and Bucherer-Bergs reaction as key steps. Their activity as sphingosine 1-phosphate receptor type 1 (S1P1) agonists were evaluated by [γ-35S] GTP binding assay. Among the thioether substituted compounds, compound 10 showed good activity as S1P1 agonist at low micromolar concentration (EC50 = 0.698 μmol/L). The result suggested that it has potential activity against autoimmune diseases and immunosuppressant of organ transplantations.

Synthesis and Biological Evaluation of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1) Inhibitors Based on a Thieno[2,3-d]pyrimidin-4(3H)-one Core

2009 ◽  
Vol 52 (21) ◽  
pp. 6660-6671 ◽  
Author(s):  
Annamaria Lilienkampf ◽  
Sampo Karkola ◽  
Sari Alho-Richmond ◽  
Pasi Koskimies ◽  
Nina Johansson ◽  
...  
Keyword(s):  
Hydroxysteroid Dehydrogenase ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation of new 4-(4-substituted-anilino)quinoline derivatives as anticancer agents

2017 ◽  
Vol 26 (5) ◽  
pp. 929-939 ◽  
Author(s):  
Khaled R. A. Abdellatif ◽  
Eman K. A. Abdelall ◽  
Mohamed A. Abdelgawad ◽  
Dina M. E. Amin ◽  
Hany A. Omar
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Quinoline Derivatives ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation
Sign in / Sign up

Export Citation Format

Share Document