Open Access
Open access
International Journal of Molecular Sciences, volume 22, issue 21, pages 11959

Synthesis and Characterization of Bis-Triazolyl-Pyridine Derivatives as Noncanonical DNA-Interacting Compounds

Anna Di Porzio 1
Ubaldina Galli 2
Pasquale Zizza 3
Sara Iachettini 3
Simona Marzano 1
Federica Santoro 1
Diego Brancaccio 1
Alfonso Carotenuto 1
Stefano De Tito 4, 5
Annamaria Biroccio 3
Bruno Pagano 1
Antonio Randazzo 1
Show full list: 15 authors
Publication typeJournal Article
Publication date2021-11-04
scimago Q1
SJR1.179
CiteScore8.1
Impact factor4.9
ISSN16616596, 14220067
Catalysis
Organic Chemistry
Inorganic Chemistry
Physical and Theoretical Chemistry
Computer Science Applications
Spectroscopy
Molecular Biology
General Medicine
Abstract

Besides the well-known double-helical conformation, DNA is capable of folding into various noncanonical arrangements, such as G-quadruplexes (G4s) and i-motifs (iMs), whose occurrence in gene promoters, replication origins, and telomeres highlights the breadth of biological processes that they might regulate. Particularly, previous studies have reported that G4 and iM structures may play different roles in controlling gene transcription. Anyway, molecular tools able to simultaneously stabilize/destabilize those structures are still needed to shed light on what happens at the biological level. Herein, a multicomponent reaction and a click chemistry functionalization were combined to generate a set of 31 bis-triazolyl-pyridine derivatives which were initially screened by circular dichroism for their ability to interact with different G4 and/or iM DNAs and to affect the thermal stability of these structures. All the compounds were then clustered through multivariate data analysis, based on such capability. The most promising compounds were subjected to a further biophysical and biological characterization, leading to the identification of two molecules simultaneously able to stabilize G4s and destabilize iMs, both in vitro and in living cells.

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