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Issue 6, 2011
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(Carboxydiamine)Pt(II) complexes of a combretastatin A-4 analogous chalcone: the influence of the diamine ligand on DNA binding and anticancer effects

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Abstract

The combretastatin A-4 analogue m-hydroxychalcone 2 was esterified with a (1-carboxyethane-2,3-diamine)dichloridoplatinum(II) fragment to give complex 6 which was more active against various cancer cell lines (IC50 < 1 µM) than its analogue 3 bearing a 6-aminomethylnicotinate ligand. Complex 6 bound to the same sites of DNA as cisplatin but caused a larger DNA unwinding angle and ten times more interstrand cross-links. Also, DNA lesions due to binding of 6 were only half as efficiently repaired as cisplatin–DNA adducts. Complex 6 also showed a much lower affinity to the platinum detoxifier glutathione.

Graphical abstract: (Carboxydiamine)Pt(ii) complexes of a combretastatin A-4 analogous chalcone: the influence of the diamine ligand on DNA binding and anticancer effects

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Publication details

The article was received on 10 Feb 2011, accepted on 08 Mar 2011 and first published on 30 Mar 2011


Article type: Concise Article
DOI: 10.1039/C1MD00042J
Med. Chem. Commun., 2011,2, 493-499

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    (Carboxydiamine)Pt(II) complexes of a combretastatin A-4 analogous chalcone: the influence of the diamine ligand on DNA binding and anticancer effects

    M. Zoldakova, B. Biersack, H. Kostrhunova, A. Ahmad, S. Padhye, F. H. Sarkar, R. Schobert and V. Brabec, Med. Chem. Commun., 2011, 2, 493
    DOI: 10.1039/C1MD00042J

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