scholarly journals Synthesis, Design, and Structure–Activity Relationship of the Pyrimidone Derivatives as Novel Selective Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase

Molecules ◽  
2018 ◽  
Vol 23 (6) ◽  
pp. 1254 ◽  
Author(s):  
Le Xu ◽  
Wenjie Li ◽  
Yanyan Diao ◽  
Hongxia Sun ◽  
Honglin Li ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Dihydroorotate Dehydrogenase ◽  
Selective Inhibitors ◽  
Synthesis Design ◽  
Structure Activity ◽  
Relationship Of

scholarly journals New Selective Inhibitors of Steroid 11β-Hydroxylation in the Adrenal Cortex. Synthesis and Structure−Activity Relationship of Potent Etomidate Analogues

2008 ◽  
Vol 51 (23) ◽  
pp. 7652-7652
Author(s):  
Ilse M. Zolle ◽  
Michael L. Berger ◽  
Friedrich Hammerschmidt ◽  
Stefanie Hahner ◽  
Andreas Schirbel ◽  
...  
Keyword(s):  
Adrenal Cortex ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Selective Inhibitors ◽  
Structure Activity ◽  
Relationship Of

scholarly journals Structural Optimization and Structure–Activity Relationship of 4-Thiazolidinone Derivatives as Novel Inhibitors of Human Dihydroorotate Dehydrogenase

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2780
Author(s):  
Fanxun Zeng ◽  
Lina Quan ◽  
Guantian Yang ◽  
Tiantian Qi ◽  
Letian Zhang ◽  
...  
Keyword(s):  
Binding Mode ◽  
Structure Activity Relationship ◽  
Immunosuppressive Drugs ◽  
Activity Relationship ◽  
Dihydroorotate Dehydrogenase ◽  
Structure Activity ◽  
Docking Method ◽  
Ic50 Values ◽  
Relationship Of ◽  
Molecular Docking Method

Human dihydroorotate dehydrogenase (hDHODH), one of the attractive targets for the development of immunosuppressive drugs, is also a potential target of anticancer drugs and anti-leukemic drugs. The development of promising hDHODH inhibitors is in high demand. Based on the unique binding mode of our previous reported 4-thiazolidinone derivatives, via molecular docking method, three new series 4-thiazolidinone derivatives were designed and synthesized as hDHODH inhibitors. The preliminary structure–activity relationship was investigated. Compound 9 of biphenyl series and compound 37 of amide series displayed IC50 values of 1.32 μM and 1.45 μM, respectively. This research will provide valuable reference for the research of new structures of hDHODH inhibitors.

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