title: Cytotoxic activities and DNA binding properties of 1-methyl-7H-indeno[1,2-b]quinolinium-7-(4-dimethylamino) benzylidene triflate.
abstract: The interaction of calf thymus DNA (ct-DNA) with a novel synthesized pyrazolo[1,5-a]indole compound 1-methyl-7H-indeno[1,2-b]quinolinium-7-(4-dimethylamino) benzylidene triflate (MIDBT) was extensively studied by various spectroscopic techniques, viscosity measurements, and gel electrophoresis. The UV-visible observation implied that the compound interacted with ct-DNA by two binding modes, intercalating into the DNA base pairs and attaching to the helix exterior of DNA. The results of the fluorescent quenching and viscosity measurements showed that MIDBT could intercalate into DNA base pairs deeply in a classical intercalative mode. Circular dichroism results showed that the binding of MIDBT shifted ct-DNA conformation from B to A at low concentrations. In the gel electrophoresis, the compound was found to promote the cleavage of plasmid pBR 322 DNA effectively. Furthermore, cytotoxic studies of this compound against eleven selected tumor cell lines have been done. The values of 50% cytotoxic concentration (IC(50)) were in the range of 1.09-18.84 μM, exhibiting the potent cytotoxic properties.
authors.affiliation: College of Pharmaceutical Sciences, Soochow University, Suzhou, China.
authors.forename: Wen
authors.initials: W
authors.lastname: Li
authors.forename: Yuan Yuan
authors.initials: YY
authors.lastname: Ji
authors.forename: Jian Wen
authors.initials: JW
authors.lastname: Wang
authors.forename: Yong Ming
authors.initials: YM
authors.lastname: Zhu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000378:metabolism* / Q000494:pharmacology*; D001597:Benzylidene Compounds / Q000378:metabolism* / Q000494:pharmacology*; D002417:Cattle; D045744:Cell Line, Tumor; D004247:DNA / Q000378:metabolism*; D053837:DNA Cleavage / Q000187:drug effects; D004996:Ethidium / Q000378:metabolism; D006801:Humans; D014783:Viscosity
chemical_list: C574889:1-methyl-7H-indeno(1,2-b)quinolinium-7-(4-dimethylamino)benzylidene triflate; D000970:Antineoplastic Agents; D001597:Benzylidene Compounds; D004247:DNA; D004996:Ethidium