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We have synthesized fourteen 3-phenylcoumarin derivatives and evaluated their anti-HIV activity. Antiviral activity was assessed on MT-2 cells infected with viral clones carrying the luciferase gene as reporter. Inhibition of HIV transcription and Tat function were tested on cells stably transfected with the HIV-LTR and Tat protein. Six compounds displayed NF-<em>κ</em>B inhibition, four resulted Tat antagonists and three of them showed both activities. Three compounds inhibited HIV replication with IC<sub>50</sub> values < 25 µM. The antiviral effect of the 4-hydroxycoumarin derivative <strong>19</strong> correlates with its specific inhibition of Tat functions, while compound <strong>8</strong>, 3-(2-chlorophenyl)coumarin, seems to act through a mechanism unrelated to the molecular targets considered in this research.