Phenanthridine derivatives as potential HIV-1 protease inhibitors.

ABSTRACT: In the present study, the antiviral activity of phenanthridine derivatives was assessed. In total, the inhibitory effect of eight structurally similar low-molecular-weight hydrophobic compounds on HIV-1 protease (HIVp) was investigated. HIVp is a key enzyme in the HIV-1 life cycle. Surface plasmon resonance technology was used for affinity assessment of compounds binding with either monomeric or dimeric forms of HIVp. HIVp enzyme inhibition assays with chromogenic substrate VII were also used to determine the IC₅₀ values. The most potent compound was 3,3,9,9-tetramethyl-3,4,9,10-tetrahydro-2H,8H-phenanthridine-1,7-dione which binds to monomeric and dimeric forms of HIVp (apparent dissociation constant, 2-7 µM; IC₅₀, 36 µМ), while possessing the most favorable Absorpti

SUBMITTER: Ershov PV 

PROVIDER: S-EPMC7605122 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature