Synthesis and structure elucidation of a cobalt(II) complex as topoisomerase I inhibitor: In vitro DNA binding, nuclease and RBC hemolysis

Ahmad, Musheer ; Afzal, Mohd. ; Tabassum, Sartaj ; Kalińska, Bożena ; Mrozinski, Jerzy ; Bharadwaj, Parimal K. (2014) Synthesis and structure elucidation of a cobalt(II) complex as topoisomerase I inhibitor: In vitro DNA binding, nuclease and RBC hemolysis European Journal of Medicinal Chemistry, 74 . pp. 683-693. ISSN 0223-5234

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Official URL: http://doi.org/10.1016/j.ejmech.2013.10.025

Related URL: http://dx.doi.org/10.1016/j.ejmech.2013.10.025

Abstract

Metal-based cancer chemotherapeutic agent of the type Co(II) complex [Co(mpca)2]·H2O (1), where, Hmpca = 9-methyl-[1,10]phenanthroline-2-carboxylic acid was synthesized and characterized by various spectroscopic and analytical techniques and further authenticated by single crystal X-ray diffraction methods. In vitro DNA binding studies of complex 1 with CT DNA was carried out by several biophysical techniques in accordance with molecular docking technique which revealed that 1 binds to DNA via intercalation mode having GC-rich sequences. Complex 1 cleaves pBR322 DNA via hydrolytic pathway (validated by T4 DNA ligase assay). Furthermore, complex 1 exhibits significant inhibitory effects on the catalytic activity of Topo-I at 25 μM concentration and further validated by molecular docking studies.

Item Type:Article
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ID Code:133555
Deposited On:29 Dec 2022 06:09
Last Modified:29 Dec 2022 06:09

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