Novel 3-O-Acyl Mesquitol Analogues as Free-Radical Scavengers and Enzyme Inhibitors: Synthesis, Biological Evaluation and Structure—Activity Relationship.

ChemInform ◽  
2003 ◽  
Vol 34 (50) ◽  
Author(s):  
R. Jagadeeshwar Rao ◽  
Ashok K. Tiwari ◽  
U. Sampath Kumar ◽  
S. Venkat Reddy ◽  
Amtul Z. Ali ◽  
...  
Keyword(s):  
Free Radical ◽  
Enzyme Inhibitors ◽  
Structure Activity Relationship ◽  
Biological Evaluation ◽  
Free Radical Scavengers ◽  
Activity Relationship ◽  
Radical Scavengers ◽  
Structure Activity

Novel C-9, 9'-O-acyl Esters of (-)-Carinol as Free-radical Scavengers and Xanthine Oxidase Enzyme Inhibitors: Synthesis and Biological Evaluation

2013 ◽  
Vol 9 (1) ◽  
pp. 100-103 ◽  
Author(s):  
Praveen Kumar Suryadevara ◽  
Hari Babu Tatipaka ◽  
Rama Subba Rao Vidadala ◽  
Ashok k Tiwari ◽  
Janaswamy Madhusudana Rao ◽  
...  
Keyword(s):  
Free Radical ◽  
Xanthine Oxidase ◽  
Enzyme Inhibitors ◽  
Biological Evaluation ◽  
Free Radical Scavengers ◽  
Radical Scavengers ◽  
Oxidase Enzyme ◽  
Synthesis And Biological Evaluation

Novel C-9, 9'-O-acyl Esters of (-)-Carinol as Free-radical Scavengers and Xanthine Oxidase Enzyme Inhibitors: Synthesis and Biological Evaluation

2012 ◽  
Vol 9 (1) ◽  
pp. 100-103
Author(s):  
Praveen Kumar Suryadevara ◽  
Hari Babu Tatipaka ◽  
Rama Subba Rao Vidadala ◽  
Ashok k Tiwari ◽  
Janaswamy Madhusudana Rao ◽  
...  
Keyword(s):  
Free Radical ◽  
Xanthine Oxidase ◽  
Enzyme Inhibitors ◽  
Biological Evaluation ◽  
Free Radical Scavengers ◽  
Radical Scavengers ◽  
Oxidase Enzyme ◽  
Synthesis And Biological Evaluation

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.

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