Related Experiment Video
Updated: Aug 26, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis, topoisomerase I inhibition and structure-activity relationship study of 2,4,6-trisubstituted pyridine
Long-Xuan Zhao1, Yoon-Soo Moon, Arjun Basnet
1Department of Chemistry, Liaoning Normal University, Dalian, Liaoning 116-029, PR China.
Abstract:
For the development of new anticancer agents, phenyl, 2-pyridyl, 2-furyl, 2-thienyl, 2-furylvinyl and 2-thienylvinyl substituted derivatives on 2,4,6-position in pyridine moiety were prepared and evaluated for their topoisomerase I inhibitory activity. Among the thirteen prepared compounds, four compounds exhibited strong topoisomerase I inhibitory activity. A structure-activity relationship study indicated that the 2-thienyl-4-furylpyridine skeleton was important for topoisomerase I inhibitory activity.
Related Concept Videos
Inhibitors of Bacterial DNA Synthesis
DNA Topoisomerases
Types and Mechanism of action
Topoisomerases are divided into two main types. Type I...
Directing and Steric Effects in Disubstituted Benzene Derivatives
Allosteric Proteins-ATCase
Aspartate transcarbamoylase (ATCase) is a cytosolic enzyme that catalyzes the condensation of L-aspartate and carbamoyl phosphate to N-carbamoyl-L-aspartate. This reaction is the first step in pyrimidine biosynthesis. UTP and CTP, the end products of the pyrimidine synthesis pathway,...
ortho–para-Directing Activators: –CH3, –OH, –⁠NH2, –OCH3
Basicity of Heterocyclic Aromatic Amines
