The long process of HIV-1 integrase inhibitor discovery and development can be attributed
to both the complexity of HIV-1 integration and poor 'integration'of these researches into …

Quinolones are among the most common frameworks present in the bioactive molecules
and hence represent an attractive starting point for the design of combinatorial libraries …

Recently, we reported small-molecule chalcones as a novel class of HIV-1 integrase (IN)
inhibitors. The most potent compound showed an IC50 value of 2μM for both IN-mediated …

We report herein the synthesis of a series of 19 2-hydroxyisoquinoline-1, 3 (2 H, 4 H)-dione
derivatives variously substituted at position 7 aimed at inhibiting selectively two-metal ion …

A new series of phenanthridinone derivatives, and diketo acid analogs, as well as related
phenanthrene and anthracene diketo acids have been synthesized and evaluated as HIV …

Metalloenzymes represent an important target space for drug discovery. A limitation to the
early development of metalloenzyme inhibitors has been the lack of established structure …

We extended the previously described dynamic pharmacophore model studies of HIV-1
integrase (IN) by considering more key residues in the active site, including Mg2+. First, we …

Abstract HIV‐1 integrase (IN) catalyzes the integration of proviral DNA into the host genome,
an essential step for viral replication. Inhibition of IN catalytic activity provides an attractive …

Two decades of intensive research efforts have led to the discovery of a large number of HIV-
1 integrase (IN) inhibitors. Recently, the United States Food and Drug Administration (US …

Integrase (IN) is the newest validated target against AIDS and retroviral infections. The
remarkable activity of raltegravir (Isentress®) led to its rapid approval by the FDA in 2007 as …