Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue -, Pages 141-150Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.01.005
Keywords
Cu-II-Sn-IV phen complex; CT DNA binding; pBR322 DNA cleavage; 14 DNA ligase assay; Topo I inhibition activity; Molecular docking
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Funding
- Department of Biotechnology, New Delhi [BT/PR9205/Med/30/13/2007]
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A novel heterobimetallic Cu-II-Sn-IV complex 1 bearing bioactive 1,10-phenanthroline pharmacophore ligand scaffold was synthesized and characterized by elemental analysis, IR, UV-vis spectroscopy, Mass (ESI and FAB) and X-ray crystallography. The in vitro DNA binding studies of complex 1 with CT DNA was carried out by various biophysical and molecular docking techniques which revealed that complex 1 binds to DNA through intercalation in the minor groove having AT-rich sequences. Complex 1 exhibits high chemical nuclease activity cleaving supercoiled pBR322 DNA via hydrolytic pathway which was further evidenced by T4 DNA ligase assay. The complex 1 shows high inhibitory activity against Topo I at a very low concentration (15 mu M), suggesting that complex 1 is an efficient catalytic inhibitor of human Topo I and further validated by molecular docking studies. (C) 2012 Elsevier Masson SAS. All rights reserved.
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