377088-75-0Relevant academic research and scientific papers
Discovery of macrocyclic hydroxamic acids containing biphenylmethyl derivatives at P1′, a series of selective TNF-α converting enzyme inhibitors with potent cellular activity in the inhibition of TNF-α release
Xue,He,Corbett,Roderick,Wasserman,Liu,Jaffee,Covington,Qian,Trzaskos,Newton,Magolda,Wexler,Decicco
, p. 3351 - 3354 (2007/10/03)
SAR exploration at P1′ using an anti-succinate-based macrocyclic hydroxamic acid as a template led to the identification of several bulky biphenylmethyl P1′ derivatives which confer potent porcine TACE and anti-TNF-α cellular activities with high selectivity versus most of the MMPs screened. Our studies demonstrate for the first time that TACE has a larger S1′ pocket in comparison to MMPs and that potent and selective TACE inhibitors can be achieved by incorporation of sterically bulky P1′ residues.
Nonpeptidic SH2 inhibitors of the tyrosine kinase ZAP-70
Vu, Chi B.,Corpuz, Evelyn G.,Pradeepan, Selvaluxmi G.,Violette, Shelia,Bartlett, Catherine,Sawyer, Tomi K.
, p. 3009 - 3014 (2007/10/03)
The synthesis of a series of 1,2,4-oxadiazole analogs is discussed along with their ZAP-70 SH2 inhibitory activity. The tyrosine moiety in the original series has been replaced with nonpeptidic functional groups without a substantial loss of binding affin
