Synthesis and anti-HIV activity of new 2-thiolumazine and 2-thiouracil metal complexes

✍ Scribed by Najim A. Al-Masoudi; Basil A. Saleh; Nesreen Abdul Karim; Ahmed Y. Issa; Christoph Pannecouque

• Publisher: John Wiley and Sons
• Year: 2010
• Tongue: English
• Weight: 144 KB
• Volume: 22
• Category: Article
• ISSN: 1042-7163
• DOI: 10.1002/hc.20654

✦ Synopsis

Abstract

A series of new Cu(II), Pt(II), VO(II), Fe(II), and Co(II) complexes (1‐‐5) with 3‐methyl‐6,7‐diphenyllumazine are described. Similarly, complexes from 2‐thiouracil with Cu(II) (6,7) and Pt(II) (8) have been prepared and characterized by spectroscopic methods. All the complexes were assayed for their anti‐HIV‐1 and HIV‐2 activity by examination of their inhibition of HIV‐induced cytopathogenicity in MT‐4 cells. Compound 3 was found to be the most active inhibitor against HIV‐2 in cell culture (EC~50~ = >18.9 μ g/mL, selectivity index (SI) = 3), which provided a good lead for further optimization. Compounds 6 and 7 exhibited some activity (EC~50~ = >7.12 μ g/mL and >2.23 μ g/mL) against HIV‐1 and HIV‐2, but no selectivity was observed (SI <1). © 2010 Wiley Periodicals, Inc. Heteroatom Chem 22:44–50, 2011; View this article online at wileyonlinelibrary.com. DOI 10.1002/hc.20654