SYNTHESIS OF ANALOGS OF THE BENZODIAZEPINE RO-5-3335, ANTAGONIST OF TAT HIV-1 - BIOLOGICAL EVALUATION BY LUCIFERASE TRANSACTIVATION AND ANTIVIRAL ASSAY
A. Farese et al., SYNTHESIS OF ANALOGS OF THE BENZODIAZEPINE RO-5-3335, ANTAGONIST OF TAT HIV-1 - BIOLOGICAL EVALUATION BY LUCIFERASE TRANSACTIVATION AND ANTIVIRAL ASSAY, European journal of medicinal chemistry, 31(6), 1996, pp. 497-505
Ro 5-3335 is a benzodiazepine which is an antagonist of the Tat protei
n of HIV-1. A series of Ro 5-3335-derived compounds have been synthesi
zed in order to evaluate whether opened analogues of the benzodiazepin
e tricyclic structure possess biological activity. The analogues are c
onstituted by two aromatic rings variously substituted, linked by an a
mino acid. The activity of these compounds has been determined by the
quantification of both inhibition of Tat activity using a cell-based t
ransfection assay and inhibition of HIV replication in acutely infecte
d cells. No analogue provided a notable inhibition of Tat-dependent tr
ansactivation or any anti-HIV activity.