Synthesis of New Benzimidazole and Benzothiazole Disulfide Metal Complexes as G-quadruplex Binding Ligands

Author(s): Kawkab Saour, Dunya Lafta.

Journal Name: Anti-Cancer Agents in Medicinal Chemistry

Volume 16 , Issue 7 , 2016

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Abstract:

Compounds that can bind and stabilize non-canonical DNA structures are named quadruplex and are of interest in anticancer drug design due to their selective inhibitions of telomerase and consequent effects on cell proliferation. In this study, we report novel Co/Cu [II] complex compounds as G-quadruplex DNA binding ligands. The results from the preliminary assay indicated that the introduction of a positively charged 6-membered tail to the aromatic terminal group of benzimidazole significantly enhanced the binding affinity with the quadruplex and exhibited anti-telomerase activity. These derivatives showed significant selectivities for the telomeric quadruplex over duplex nucleic acids. The stabilization of non-canonical forms estimated with the FRET DNA technology using different sequences, such as F21T, c-kit1 and c-kit2, in cancer cell lines were assessed. Three members of this family showed to be very selective in stabilizing one particular G-quadruplex.

Keywords: Metal complex, benzimidazole, disulfide, FRET, circular dichroism, quadruplex DNA.

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Article Details

VOLUME: 16
ISSUE: 7
Year: 2016
Page: [891 - 897]
Pages: 7
DOI: 10.2174/1871520616666160204111637
Price: $58

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