2,4,6-Trisubstituted pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship.

doi:10.1016/J.BMC.2007.04.047

Paper

2,4,6-Trisubstituted pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship.

Published Jul 1, 2007 · Arjun Basnet, Pritam Thapa, Radha Karki

Bioorganic & medicinal chemistry

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108

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Abstract

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2,4,6-trisubstituted pyridines show significant topoisomerase I and II inhibitory activities and cytotoxicities against various human cancer cell lines, with 4'-pyridine at the 6-position playing a key role in biological activity.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

2,4,6-Trisubstituted pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship.

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References

Synthesis, topoisomerase I inhibition and structure-activity relationship study of 2,4,6-trisubstituted pyridine derivatives.

Four 2,4,6-trisubstituted pyridine derivatives showed strong topoisomerase I inhibitory activity, with the 2-thienyl-4-furylpyridine skeleton being crucial for their anticancer activity.

Nitro and amino substitution in the D-ring of 5-(2-dimethylaminoethyl)- 2,3-methylenedioxy-5H-dibenzo[c,h][1,6]naphthyridin-6-ones: effect on topoisomerase-I targeting activity and cytotoxicity.

Nitro substituents in the D-ring of 5-(2-dimethylaminoethyl)- 2,3-methylenedioxy-5H-dibenzo[c,h][1,6]naphthyridin-6-ones retain their TOP1-targeting activity and

Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2':6',2"-, 2,2':6',3"- and 2,2':6',4"-terpyridine derivatives.

2,2′:6′,2′′-terpyridine derivatives show high cytotoxicity against human tumor cells and are potent topoisomerase I inhibitors, offering potential as new anticancer agents.

Human DNA-Topoisomerases – Diagnostic and Therapeutic Implications for Cancer

Topoisomerase inhibitors, which disrupt DNA topology, are crucial for cancer cell survival and can lead to DNA single-strand breaks, causing cell death.

The Design and Synthesis of Bis-[4′-Azido-2,2′:6′,2″-Terpyridine Platinum(II)] Complexes with Rigid and Extended Linkers for Studying the Topology of DNA by Photoaffinity Labeling☆

Bis-[4′-Azido-2,2′:6′,2′′-terpyridine platinum(II)] complexes with linear linkers of varying lengths can study DNA topology by photoaffinity labeling, allowing for 2D gel electrophoresis analysis.

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