869099-06-9Relevant academic research and scientific papers
Structure-activity relationship of ortho- and meta-phenol based LFA-1 ICAM inhibitors
Lin, Edward Yin-Shiang,Guckian, Kevin M.,Silvian, Laura,Chin, Donovan,Ann Boriack-Sjodin,van Vlijmen, Herman,Friedman, Jessica E.,Scott, Daniel M.
scheme or table, p. 5245 - 5248 (2009/05/08)
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.
