Repozytorium

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

Autorzy

Musheer Ahmad

Mohd Afzal

Sartaj Tabassum

Bożena Kalińska

Jerzy Mroziński

Parimal K. Bharadwaj

Rok wydania

2014

Czasopismo

European Journal of Medicinal Chemistry

Numer woluminu

74

Strony

683-693

DOI

10.1016/j.ejmech.2013.10.025

Kolekcja

Naukowa

Język

Angielski

Typ publikacji

Artykuł

Streszczenie

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.

Słowa kluczowe

CT DNA binding, pBR322 DNA cleavage, T4 DNA ligase assay, Topo I inhibition activity, Molecular docking

Adres publiczny

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

Strona internetowa wydawcy

http://www.elsevier.com

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