A promising chromone-based compounds in drug discovery for new anti-inflammatory and anti-cancer drugs

• Main Authors: Rullah, Kamal, Shamsudin, Nur Farisya
• Format: Conference or Workshop Item
• Language: English; English; English; English
• Published: 2022
• Subjects: RS403 Materia Medica-Pharmaceutical Chemistry
• Online Access: http://irep.iium.edu.my/102004/3/PDF%20%28Cover%20page%20of%20the%20abstract%20book%29%20-%20Cover%20Image.pdf; http://irep.iium.edu.my/102004/2/PDF%20%28Abstract%20page%29%20-%20Published%20Version.pdf; http://irep.iium.edu.my/102004/1/PDF%20%28Invitation%20letter%20Dr%20Kamal%20Rullah%29.pdf; http://irep.iium.edu.my/102004/4/PDF%20%28Presentation%29%20-%20Presentation.pdf; http://irep.iium.edu.my/102004/

Chromone, a group of heterocyclic compounds, has been recognised as a privileged structure for new drug discovery and development. These scaffolds have exhibited extensive acceptability due to their drug-like properties and versatile binding properties. Among several approved anti-inflammatory and anti-cancer drugs, these scaffolds show high selectivity for certain specific targets. For this reason, a significantly increasing number of research groups are interested in developing new synthetic methods and evaluating biological properties. In this view, we will discuss some of the important discoveries of chromone-based compounds as anti-inflammatory and anti-cancer agents, such as 2-(3,4-dimethoxyphenyl)-3-(4- fluorophenyl)-6-methoxy-4H-chromen-4-one (KR-1401-KW) which was found to be significantly active in suppressing PGE2-associated inflammatory responses and 3-(4-(chloromethyl)phenyl)-2-(3,4- dimethoxyphenyl)-7-methoxy-4H-chromen-4-one which was displayed potential inhibitor of UNC-51-like kinase 1 (ULK1) (KR-2201-NF) modulates autophagy and induces apoptosis in colon cancer. Moreover, computational evidence, including docking and molecular dynamics (MD) simulations, makes the compounds promising candidates for new anti-inflammatory and anti-cancer drugs.