title: Synthesis and binding studies of novel di-substituted phenanthroline compounds with genomic promoter and human telomeric DNA G-quadruplexes.
abstract: Six novel di-substituted phenanthroline derivatives 5a-7a and 3b-5b have been prepared, and their binding interactions with human telomeric (h-telo) and promoter (c-kit2 and c-myc) G-quadruplex DNAs were investigated. All the compounds are potent stabilisers of the G-quadruplex structures and compounds 3b, 4b, and 5b exhibit high G-quadruplex DNA selectivity over duplex DNA. The binding affinities of these compounds to G-quadruplex DNA are higher than to duplex DNA. CD spectra show that the compound can induce the formation of an anti-parallel structure of the h-telo G-quadruplex. Each h-telo quadruplex binds two compound molecules by the end-stacking mode. Six new compounds are able to inhibit significantly the telomerase activity at low μM concentration.
authors: Key Laboratory of Chemical Biology and Molecular Engineering of Ministry of Education, Institute of Molecular Science, Shanxi University, Taiyuan 030006, PR China. weichuny@sxu.edu.cn
authors: Chunying
authors: C
authors: Wei
authors: Yanbo
authors: Y
authors: Wang
authors: Meiying
authors: M
authors: Zhang
mesh_terms: D002942:Circular Dichroism; D054856:G-Quadruplexes; D006801:Humans; D008958:Models, Molecular; D061848:Optical Imaging; D010618:Phenanthrolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D016133:Polymerase Chain Reaction; D011401:Promoter Regions, Genetic; D013054:Spectrophotometry, Atomic; D016615:Telomere / Q000737:chemistry*
chemical_list: D010618:Phenanthrolines