Ashley E. Fenwick

3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).

Potent 3-anilino-4-arylmaleimide glycogen synthase kinase-3 (GSK-3) inhibitors have been prepared using automated array methodology. A number of these are highly selective, having little inhibitory potency against more than 20 other protein kinases.

Inhibition of human cytomegalovirus protease by enedione derivatives of thieno[2,3-d]oxazinones through a novel dual acylation/alkylation mechanism

Enedione derivatives of thieno[2,3-d]oxazinones are nanomolar inhibitors of CMV protease which act through a novel dual acylation of the catalytic serine and alkylation of the protease cysteine 161 via a Michael addition to the enedione moiety of the inhibitor.

Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K

Using solid-phase synthesis, a library of novel cyclic alkoxyketones has been constructed which show strong inhibitory activity against the cysteine protease, cathepsin K (EC 3.4.22.38).

Diastereoselective synthesis, activity and chiral stability of cyclic alkoxyketone inhibitors of cathepsin K.

The diastereoselective synthesis of a novel class of cathepsin K inhibitors together with their cathepsin K affinity and stability towards aqueous buffer is reported.

Synthesis of analogues of arachidonic acid as potential inhibitors of leukotriene biosynthesis

A versatile route to 1,2-disubstituted aromatic analogues of arachidonic acid of formulae (5) and (6) has been established involving the stepwise cross-coupling of alkynes to 1,2-dibromobenzene. Subsequent reduction allows good control over the degree of unsaturation and the stereochemistry of the resulting alkenes. Some of these compounds have been shown to inhibit the biosynthesis of leukotrienes in vitro.