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

Synthesis and anti‐HIV activity of new 2‐thiolumazine and 2‐thiouracil metal complexes 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 (EC50 = >18.9 μ g/mL, selectivity index (SI) = 3), which provided a good lead for further optimization. Compounds 6 and 7 exhibited some activity (EC50 = >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 http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Heteroatom Chemistry Wiley

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

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References (30)

Publisher
Wiley
Copyright
Copyright © 2010 Wiley Periodicals, Inc.
ISSN
1042-7163
eISSN
1098-1071
DOI
10.1002/hc.20654
Publisher site
See Article on Publisher Site

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 (EC50 = >18.9 μ g/mL, selectivity index (SI) = 3), which provided a good lead for further optimization. Compounds 6 and 7 exhibited some activity (EC50 = >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

Journal

Heteroatom ChemistryWiley

Published: Jan 1, 2011

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