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Design and synthesis of heterobimetallic topoisomerase I and II inhibitor complexes: In vitro DNA binding, interaction with 5′-GMP and 5′-TMP and cleavage studies

Paper ID Volume ID Publish Year Pages File Format Full-Text
30963 44522 2010 10 PDF Available
Title
Design and synthesis of heterobimetallic topoisomerase I and II inhibitor complexes: In vitro DNA binding, interaction with 5′-GMP and 5′-TMP and cleavage studies
Abstract

New potential cancer chemotherapeutic complexes Cu–Sn2/Zn–Sn23 and 4 were designed and prepared as topoisomerases inhibitors; their in vitro DNA binding studies were carried out which reveal strong electrostatic binding via phosphate backbone of DNA helix, in addition to other binding modes viz. coordinate covalent and partial intercalation. To throw insight to molecular binding event at the target site, UV–vis titrations of 3 and 4 with mononucleotides of interest, viz, 5′-GMP and 5′-TMP were carried out, (in case of 4) by 1H and 31P NMR. Cleavage studies employing gel electrophoresis demonstrate both the complexes 3 and 4 are efficient cleavage agents and are specific groove binders (complex 3 binds to both major and minor groove while complex 4 is specifically minor groove binder only). In addition, the complexes show high inhibition activity against topoisomerase I and II. However, complex 4 exhibits significant inhibitory effects on the Topo I activity at a very low concentration ∼2.5 μM.

Keywords
Heterobimetallic complexes; In vitro binding studies; 5′-GMP; 5′-TMP; Cleavage studies; Topoisomerases inhibition
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Design and synthesis of heterobimetallic topoisomerase I and II inhibitor complexes: In vitro DNA binding, interaction with 5′-GMP and 5′-TMP and cleavage studies
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Publisher
Database: Elsevier - ScienceDirect
Journal: Journal of Photochemistry and Photobiology B: Biology - Volume 101, Issue 1, 5 October 2010, Pages 37–46
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
Get Full-Text Now
Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
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