Naphthalenediimide-Linked Bisbenzimidazole Derivatives as Telomeric G-Quadruplex-Stabilizing Ligands with Improved Anticancer Activity.

ABSTRACT: Human telomeric G-quadruplex DNA stabilization has emerged as an exciting novel approach for anticancer drug development. In the present study, we have designed and synthesized three C₂-symmetric bisubstituted bisbenzimidazole naphthalenediimide (NDI) ligands, ALI-C₃ , BBZ-ARO, and BBZ-AROCH₂ , which stabilize human telomeric G-quadruplex DNA with high affinity. Herein, we have studied the binding affinities and thermodynamic contributions of each of these molecules with G-quadruplex DNA and compared the same to those of the parent NDI analogue, BMSG-SH-3. Results of fluorescence resonance energy transfer and surface plasmon resonance demonstrate that these ligands have a higher affinity for G₄-DNA over d

SUBMITTER: Sur S 

PROVIDER: S-EPMC6044781 | biostudies-literature | 2017 Mar

REPOSITORIES: biostudies-literature