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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
chemistry
Molecular drug design, synthesis and crystal structure determination of Cu
II
-Sn
IV
heterobimetallic core: DNA binding and cleavage studies
European Journal of Medicinal Chemistry, Volume 49, Year 2012
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Description
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 μM), suggesting that complex 1 is an efficient catalytic inhibitor of human Topo I and further validated by molecular docking studies. © 2012 Elsevier Masson SAS. All rights reserved.
Authors & Co-Authors
Arjmand, Farukh
India, Aligarh
Aligarh Muslim University
Parveen, Shazia
India, Aligarh
Aligarh Muslim University
Afzal, Mohammad P.
India, Aligarh
Aligarh Muslim University
Toupet, Loïc J.
France, Rennes
Institut de Physique de Rennes
Ben Hadda, Taibi
Morocco, Oujda
Université Mohammed Premier Oujda
Statistics
Citations: 72
Authors: 5
Affiliations: 3
Identifiers
Doi:
10.1016/j.ejmech.2012.01.005
ISSN:
02235234
e-ISSN:
17683254
Research Areas
Genetics And Genomics