Related Experiment Video
Updated: Oct 7, 2025

High-throughput Identification of Synergistic Drug Combinations by the Overlap2 Method
Published on: May 21, 2018
Recent Developments of Coumarin-based Hybrids in Drug Discovery
Dongguo Xia1, Hao Liu1, Xiang Cheng1
1School of Science, Anhui Agricultural University, Hefei, 230036, China.
Abstract:
Coumarin scaffold is a highly significant O-heterocycle, namely benzopyran-2-ones, which form an elite class of naturally occurring compounds with promising therapeutic perspectives. Based on its broad spectrum of biological activities, the privileged coumarin scaffold is applied to medicinal and pharmacological treatments by several rational design strategies and approaches. Structure-activity relationships of the coumarin-based hybrids with various bioactivity fragments revealed significant information toward the further development of highly potent and selective disorder therapeutic agents. The molecular docking studies between coumarins and critical therapeutic enzymes demonstrated a mode of action by forming noncovalent interactions with more than one receptor, further rationally confirming information about structure-activity relationships. This review summarizes recent developments related to coumarin-based hybrids with other pharmacophores aiming at numerous feasible therapeutic enzymatic targets in order to combat various therapeutic fields, including anticancer, antimicrobic, anti-Alzheimer, anti-inflammatory activities.
Related Concept Videos
Drug Discovery: Overview
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
Anticoagulant Drugs: Low-Molecular-Weight Heparins
Therapeutic Drug Monitoring: Overview and Classification
Anticoagulant Drugs: Vitamin K Antagonists and Direct Oral Anticoagulants
Warfarin, a prominent vitamin K antagonist family member, exerts its effect by inhibiting the enzyme VKORC1 (vitamin K epoxide reductase complex 1). By hindering this enzyme, warfarin...
Cardiovascular Drugs: Classification based on Therapeutic Indications

