title: Synthesis of New Benzimidazole and Benzothiazole Disulfide Metal Complexes as G-quadruplex Binding Ligands.
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.
authors: Kawkab
authors: K
authors: Saour
authors: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Kufa University, P.O. Box: 21, AL-Najaf, Iraq. dunyal.mohammed@uokufa.edu.iq.
authors: Dunya
authors: D
authors: Lafta
mesh_terms: D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry; D052160:Benzothiazoles / Q000138:chemical synthesis* / Q000737:chemistry; D002460:Cell Line; D045744:Cell Line, Tumor; D031541:Fluorescence Resonance Energy Transfer; D054856:G-Quadruplexes; D006801:Humans; D008024:Ligands
chemical_list: D001562:Benzimidazoles; D052160:Benzothiazoles; D008024:Ligands