Kim, Mi Kyoung Yu, Mi-Sun Park, Hye Ri Kim, Kyung Bo Lee, Chaewoon Cho, Suh Young Kang, Jihoon Yoon, Hyunjun Kim, Dong-Eun Choo, Hyunah Jeong, Yong-Joo Chong, Youhoon 2024-01-20T16:02:42Z 2024-01-20T16:02:42Z 2021-09-05 2011-11 0223-5234 https://pubs.kist.re.kr/handle/201004/129851 In this study, as a bioisosteric alternative scaffold of the antiviral aryl diketoacids (ADKs), we used 5-hydroxychromone on which two arylmethyloxy substituents were installed. The 5-hydroxychromones (5b-5g) thus prepared showed anti-HCV activity and, depending on the aromatic substituents on the 2-arylmethyloxy moiety, some of the derivatives (5b-5f) were also active against SCV. In addition, unlike the ADKs which showed selective inhibition against the helicase activity of the SCV NTPase/helicase, the 5-hydroxychromones (5b-5f) were active against both NTPase and helicase activities of the target enzyme. Among those, 3-iodobenzyloxy-substituted derivative 5e showed the most potent activity against HCV (EC50 = 4 mu M) as well as SCV (IC50 = 4 mu M for ATPase activity, 11 mu M for helicase activity) and this might be used as a platform structure for future development of the multi-target or broad-spectrum antivirals. (C) 2011 Elsevier Masson SAS. All rights reserved. English ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER INHIBITORS ACID SITE 2,6-Bis-arylmethyloxy-5-hydroxychromones with antiviral activity against both hepatitis C virus (HCV) and SARS-associated coronavirus (SCV) Article 10.1016/j.ejmech.2011.09.005 1 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.46, no.11, pp.5698 - 5704 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 46 11 5698 5704 scie scopus 000298120500051 2-s2.0-80054944870 Chemistry, Medicinal Pharmacology & Pharmacy Article INHIBITORS ACID SITE Aryl diketoacid (ADK) 5-Hydroxyflavone 5-Hydroxychromone Hepatitis C Severe Acute Respiratory Syndrome (SARS)