The modulation of gene expression by nuclear receptors has considerable potential in cardiovascular disease therapy. For example, cholesterol-lipid metabolism is partly regulated by the production of several proteins involved in cholesterol efflux from cells. Control of gene expression and hence production of these proteins is exerted by liver X receptors (LXRs) which have various oxidized sterols as their endogenous agonists. In order to modulate gene expression via LXRs, we have targeted novel LXR agonists leading to the identification of a series of high affinity LXR agonists with excellent functional activity. This series of agonists incorporates amides on a quinoline core. We will present the syntheses, biological activity and SAR of these ligands.