Work

9,10-Bis[(4-(2-hydroxyethyl)piperazine-1-yl)prop2-yne-1-yl]anthracene: G-Quadruplex Selectivity and Anticancer Activity

Year: 2024

Type: article

Abstract: G-Quadruplexes (G4s) are appealing targets for anticancer therapy because of their location in the genome and their role in regulating physiological and pathological processes. In this article, we report the characterization of the molecular interaction and selectivity of OAF89, a 9,10-disubstituted G4-binding anthracene derivative, with different DNA sequences. Advanced analytical methods, including mass spectrometry and nuclear magnetic resonance, were used to conduct the investigation, together with the use of in silico docking and molecular dynamics. Eventually, the compound was tested in vitro to assess its bioactivity against lung cancer cell lines.

Source: ACS Medicinal Chemistry Letters

DOI: 10.1021/acsmedchemlett.4c00340

Authors: Margrate Anyanwu, Matteo Giannangeli, Xing-Xing Fan, Paolo Coghi, Giovanni Ribaudo, Alessandra Gianoncelli

Institutions: University of Brescia, Macau University of Science and Technology

Language: English

Topic: DNA and Nucleic Acid Chemistry

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

Funders: Università degli Studi di Brescia, Regione Lombardia