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Synthesis and HCV NS3 serine protease inhibitory activity of P2–P4 macrocyclic inhibitors and SAR around this macrocyclic core is described in this communication. X-ray structure of inhibitor 38 bound to the protease is discussed.
Three new perylene derivatives with branched ionizable side chains were investigated for their G-quadruplex binding specificities, in comparison with two well-studied G-quadruplex ligands: PIPER and TmPyP 4 .
A novel series of GlyT-1 inhibitors is described. The most potent compound, 38 , has a GlyT-1 b IC 50 = 59 nM. In vitro and in vivo assessment of CNS penetration showed that lead compounds had poor CNS exposure most likely due to active efflux by PgP transporters.
A new azanucleoside with anti-HIV activity.
We report the synthesis and biochemical evaluation of a range of benzyl imidazole-based compounds which have been targeted against the two components of this enzyme, that is, 17α-hydroxylase (17α-OHase) and 17,20-lyase (lyase).
Synthesis and SAR of substituted pyrrolotriazine-4-one analogues as Eg5 inhibitors are described. Analogue 26 demonstrated in vivo efficacy in an iv P388 murine leukemia model.
The inhibitory activity of several benzalphthalides, phthalazin-1-ones, imidazo(2,1- a )isoindoles and pyrimido(2,1- a )isoindoles on NF-κB, Tat and HIV replication is evaluated.
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