Design and synthesis of EGFR dimerization inhibitors and evaluation of their potential in the treatment of psoriasis

…, RJ Anderson, A Cunningham, SE George…

Index: Petch, Donna; Anderson, Rosaleen J.; Cunningham, Anne; George, Suja E.; Hibbs, David E.; Liu, Ran; MacKay, Simon P.; Paul, Andrew; Small, David A.P.; Groundwater, Paul W. Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 19 p. 5901 - 5914

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Citation Number: 14

Abstract

Hit compounds from in silico screening for inhibitors of the EGFR dimerization process were evaluated for their anti-proliferative (CCD-1106 keratinocytes) and anti-oxidant (TBA assay) activity and their effect on EGFR dimerization (BS3 chemical crosslinking assay). 7-Benzyl-8- {N′-[1-(3-ethoxy-4-hydroxyphenyl) meth-(Z)-ylidene] hydrazino}-1, 3-dimethylxanthine 2a (127μM) leads to 37% inhibition of p-EGFR dimerization in the CCD-1106 cell line and ...