title: Promoting the formation and stabilization of human telomeric G-quadruplex DNA, inhibition of telomerase and cytotoxicity by phenanthroline derivatives.
abstract: Four new di-substituted phenanthroline-based compounds a-d have been designed and prepared, and they have been shown to induce the formation of anti-parallel structure of human telomeric G-quadruplex DNA by CD spectra. FRET assay indicates that the melting temperature increases (ΔT(m) values) of G-quadruplex in buffer (pH 7.4) containing 100 mM NaCl are 31.6, 34.6, 17.8 and 32.6 °C for the compounds (1.0 μM) a, b, c and d, respectively. Competitive FRET assay shows that the four compounds exhibit a high G-quadruplex DNA selectivity over duplex DNA. Three of the compounds are the potent telomerase inhibitors and HeLa cell proliferation inhibitors.
authors.affiliation: Key Laboratory of Chemical Biology and Molecular Engineering of Ministry of Education, Institute of Molecular Science, Shanxi University, Taiyuan, 030006, China.
authors.forename: Lihua
authors.initials: L
authors.lastname: Wang
authors.forename: Ye
authors.initials: Y
authors.lastname: Wen
authors.forename: Jie
authors.initials: J
authors.lastname: Liu
authors.forename: Jun
authors.initials: J
authors.lastname: Zhou
authors.forename: Can
authors.initials: C
authors.lastname: Li
authors.forename: Chunying
authors.initials: C
authors.lastname: Wei
mesh_terms: D002470:Cell Survival / Q000187:drug effects; D002474:Cell-Free System; D054856:G-Quadruplexes; D006367:HeLa Cells; D006801:Humans; D010618:Phenanthrolines / Q000737:chemistry* / Q000494:pharmacology; D019098:Telomerase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D016615:Telomere / Q000737:chemistry*
chemical_list: D010618:Phenanthrolines; D019098:Telomerase