Specific and dual antagonists of α 4 β 1 and α 4 β 7 integrins

…, T Lanza, E McCauley, G Van Riper, U Kidambi…

Index: Lin, Linus S.; Lanza Jr., Thomas; McCauley, Ermenegilda; Riper, Gail Van; Kidambi, Usha; Cao, Jin; Egger, Linda A.; Mumford, Richard A.; Schmidt, John A.; MacCoss, Malcolm; Hagmann, William K. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 2 p. 133 - 136

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Citation Number: 27

Abstract

N-(3, 5-Dichlorophenylsulfonyl)-(R)-thioprolyl biarylalanine 10a has been identified as a potent and specific antagonist of the α4β1 integrin. Altering the configuration of thioproline from R to S led to a series of dual antagonists of α4β1 and α4β7, and the N-acetyl analogue 8b was found to be the most potent dual antagonist. A binding site model for α4β1 and α4β7 is proposed to explain the structure–activity relationship.