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• W1860000541 abstract "The development of G-quadruplex (G4) DNA binding small molecules has become an important strategy for selectively targeting cancer cells. Herein, we report the design and evolution of a new kind of carbazole-based benzimidazole dimers for their efficient telomerase inhibition activity. Spectroscopic titrations reveal the ligands high affinity toward the G4 DNA with significantly higher selectivity over duplex-DNA. The electrophoretic mobility shift assay shows that the ligands efficiently promote the formation of G4 DNA even at a lower concentration of the stabilizing K(+) ions. The TRAP-LIG assay demonstrates the ligand's potential telomerase inhibition activity and also establishes that the activity proceeds via G4 DNA stabilization. An efficient nuclear internalization of the ligands in several common cancer cells (HeLa, HT1080, and A549) also enabled differentiation between normal HFF cells in co-cultures of cancer and normal ones. The ligands induce significant apoptotic response and antiproliferative activity toward cancer cells selectively when compared to the normal cells." @default.
• W1860000541 created "2016-06-24" @default.
• W1860000541 creator A5012378530 @default.
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• W1860000541 creator A5051882620 @default.
• W1860000541 creator A5090701117 @default.
• W1860000541 date "2015-01-01" @default.
• W1860000541 modified "2023-09-26" @default.
• W1860000541 title "New dimeric carbazole–benzimidazole mixed ligands for the stabilization of human telomeric G-quadruplex DNA and as telomerase inhibitors. A remarkable influence of the spacer" @default.
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• W1860000541 doi "https://doi.org/10.1039/c5ob00675a" @default.
• W1860000541 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26149178" @default.
• W1860000541 hasPublicationYear "2015" @default.
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