Halogenated pentamethine cyanine dyes exhibiting high fidelity for G-quadruplex DNA.

ABSTRACT: Design and optimization of quadruplex-specific small molecules is developing into an attractive strategy for anti-cancer therapeutics with some promising candidates in clinical trials. A number of therapeutically favorable features of cyanine molecules can be effectively exploited to develop them as promising quadruplex-targeting agents. Herein, the design, synthesis and evaluation of a series of dimethylindolenine cyanine dyes with varying halogen substitutions are reported. Their interactions with telomeric and c-myc quadruplexes as well as a reference duplex sequence have been evaluated using thermal melting, biosensor-surface plasmon resonance, circular dichroism, isothermal titration calorimetry and mass spectrometry. Thermal melting analysis indicates that these ligands exhibit signi

SUBMITTER: Nanjunda R 

PROVIDER: S-EPMC3539309 | biostudies-literature | 2012 Dec

REPOSITORIES: biostudies-literature