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ID: ALA1139661
Journal: Bioorg Med Chem Lett
Title: Arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 2: Optimization of P1 and N-aryl.
Authors: Alper PB, Liu H, Chatterjee AK, Nguyen KT, Tully DC, Tumanut C, Li J, Harris JL, Tuntland T, Chang J, Gordon P, Hollenbeck T, Karanewsky DS.
Abstract: A systematic study of anilines led to the discovery of a metabolically robust fluoroindoline replacement for the alkoxy aniline toxicophore in 1. Investigations of the P1 pocket resulted in the discovery of a wide tolerance of functionality leading to the discovery of 11 as a potent and selective inhibitor of cathepsin S.
CiteXplore: 16412634