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Title: Molecular recognition and imaging of human telomeric G-Quadruplex DNA in live cells : a systematic advancement of thiazole orange scaffold to enhance binding specificity and inhibition of gene expression
Authors: Long, W
Zheng, BX
Huang, XH
She, MT
Liu, AL
Zhang, K
Wong, WL 
Lu, YJ
Issue Date: 25-Feb-2021
Source: Journal of medicinal chemistry, 25 Feb. 2021, v. 64, no. 4, p. 2125-2138
Abstract: A series of fluorescent ligands, which were systematically constructed from thiazole orange scaffold, was investigated for their interactions with G-quadruplex structures and antitumor activity. Among the ligands, compound 3 was identified to exhibit excellent specificity toward telomere G4-DNA over other nucleic acids. The affinity of 3-Htg24 was almost 5 times higher than that of double-stranded DNA and promoter G4-DNA. Interaction studies showed that 3 may bind to both G-tetrad and the lateral loop near the 5′-end. The intracellular colocalization with BG4 and competition studies with BRACO19 reveal that 3 may interact with G4-structures. Moreover, 3 reduces the telomere length and downregulates hTERC and hTERT mRNA expression in HeLa cells. The cytotoxicity of 3 against cancer cells (IC50 = 12.7–16.2 μM) was found to be generally higher than noncancer cells (IC50 = 52.3 μM). The findings may support that the ligand is telomere G4-DNA specific and may provide meaningful insights for anticancer drug design.
Publisher: American Chemical Society
Journal: Journal of medicinal chemistry 
ISSN: 0022-2623
EISSN: 1520-4804
DOI: 10.1021/acs.jmedchem.0c01656
Rights: © 2021 American Chemical Society
This document is the Accepted Manuscript version of a Published Work that appeared in final form in Journal of Medicinal Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see
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