作者
Akash K Jain, Ananya Paul, Basudeb Maji, K Muniyappa, Santanu Bhattacharya
发表日期
2012/4/12
期刊
Journal of Medicinal Chemistry
卷号
55
期号
7
页码范围
2981-2993
出版商
American Chemical Society
简介
Ligand-induced stabilization of G-quadruplex structures formed by the human telomeric DNA is an active area of research. The compounds which stabilize the G-quadruplexes often lead to telomerase inhibition. Herein we present the results of interaction of new monomeric and dimeric ligands having 1,3-phenylene-bis(piperazinyl benzimidazole) unit with G-quadruplex DNA (G4DNA) formed by human telomeric repeat d[(G3T2A)3G3]. These ligands efficiently stabilize the preformed G4DNA in the presence of 100 mM monovalent alkali metal ions. Also, the G4DNA formed in the presence of low concentrations of ligands in 100 mM K+ adopts a highly stable parallel-stranded conformation. The G-quadruplexes formed in the presence of the dimeric compound are more stable than that induced by the corresponding monomeric counterpart. The dimeric ligands having oligo-oxyethylene spacers provide much higher …
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AK Jain, A Paul, B Maji, K Muniyappa, S Bhattacharya - Journal of Medicinal Chemistry, 2012