Author/Authors :
Edward Yin-Shiang Lin، نويسنده , , Kevin M. Guckian، نويسنده , , Laura Silvian، نويسنده , , Donovan Chin، نويسنده , , P. Ann Boriack-Sjodin، نويسنده , , Herman van Vlijmen، نويسنده , , Jessica E. Friedman، نويسنده , , Daniel M. Scott، نويسنده ,
Abstract :
LFA-1 ICAM inhibitors based on ortho- and meta-phenol templates were designed and synthesized by Mitsunobu chemistry. The selection of targets was guided by X-ray co-crystal data, and led to compounds which showed an up to 30-fold increase in potency over reference compound 1 in the LFA-1/ICAM1-Ig assay. The most active compound exploited a new hydrogen bond to the I-domain and exhibited subnanomolar potency.
