Work

Synthetic approach to a novel quinoline scaffold 4-amino-5,10-dihydropyrimido[4,5-b]quinolin-2(1H)-one with antiproliferative effects on HCT116 colon cancer cell lines

Year: 2025

Type: article

Abstract: Pyrimido-quinoline derivatives have demonstrated diverse biological activities, including anticancer, antimicrobial, anti-inflammatory, and anti-allergic properties, making them valuable scaffolds in medicinal chemistry. In this study, we developed a straightforward one-pot three-component reaction for synthesizing pyrimido[4, 5-b]quinoline-2, 4(1H, 3H)-diones and used X-ray crystallography to confirm its structure. Building on this scaffold, we designed and synthesized a cytosine-like derivative, compound 11. HPLC-based uptake assays confirmed that compound 11 could penetrate the cells. This compound exhibited antiproliferative effects in HCT116 cells after 72 hours. These findings highlight the potential of pyrimido-quinoline derivatives as a promising scaffold for drug discovery.

Source: Journal of Molecular Structure

DOI: 10.1016/j.molstruc.2025.143031

Authors: Ting Chen, Elodie Olivier, Patrick Deschamps, Syrine Mahdadi, Philippe Helissey, Stéphanie Desbène-Finck