scholarly journals Structure‐activity relationship and mode of action studies highlight 1‐(4‐biphenylylmethyl)‐1H‐imidazole derived small molecules as potent CYP121 inhibitors

ChemMedChem ◽  
2021 ◽  
Author(s):  
Sebastian Adam ◽  
Isabell Walter ◽  
Rolf Hartmann ◽  
Andreas Kany ◽  
Jesko Köhnke ◽  
...  
Keyword(s):  
Small Molecules ◽  
Mode Of Action ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity

Triazol: a privileged scaffold for proteolysis targeting chimeras

2019 ◽  
Vol 11 (22) ◽  
pp. 2919-2973 ◽  
Author(s):  
Li-Wen Xia ◽  
Meng-Yu Ba ◽  
Wei Liu ◽  
Weyland Cheng ◽  
Chao-Ping Hu ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Anticancer Activity ◽  
Mode Of Action ◽  
Critical Analysis ◽  
Enzyme Inhibitors ◽  
Structure Activity Relationship ◽  
Target Protein ◽  
Activity Relationship ◽  
Structure Activity ◽  
Privileged Scaffold

Current traditional drugs such as enzyme inhibitors and receptor agonists/antagonists present inherent limitations due to occupancy-driven pharmacology as the mode of action. Proteolysis targeting chimeras (PROTACs) are composed of an E3 ligand, a connecting linker and a target protein ligand, and are an attractive approach to specifically knockdown-targeted proteins utilizing an event-driven mode of action. The length, hydrophilicity and rigidity of connecting linkers play important role in creating a successful PROTAC. Some PROTACs with a triazole linker have displayed promising anticancer activity. This review provides an overview of PROTACs with a triazole scaffold and discusses its structure–activity relationship. Important milestones in the development of PROTACs are addressed and a critical analysis of this drug discovery strategy is also presented.

scholarly journals Antitubercular 2-Pyrazolylpyrimidinones: Structure–Activity Relationship and Mode-of-Action Studies

2021 ◽  
Author(s):  
Candice Soares de Melo ◽  
Vinayak Singh ◽  
Alissa Myrick ◽  
Sandile B. Simelane ◽  
Dale Taylor ◽  
...  
Keyword(s):  
Mode Of Action ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity

Structure–activity relationship studies of thalidomide analogs with a taxol-like mode of action

2013 ◽  
Vol 23 (24) ◽  
pp. 6902-6904 ◽  
Author(s):  
Bulbul Pandit ◽  
Zhigen Hu ◽  
Somsundaram N. Chettiar ◽  
Jennifer Zink ◽  
Zili Xiao ◽  
...  
Keyword(s):  
Mode Of Action ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity
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