Evaluation of synthetic acridones and 4-quinolinones as potent inhibitors of cathepsins L and V

…, RP Severino, D Brömme, PC Vieira, AG Corrêa

Index: Marques, Emerson F.; Bueno, Mauro A.; Duarte, Patricia D.; Silva, Larissa R.S.P.; Martinelli, Ariani M.; Dos Santos, Caio Y.; Severino, Richele P.; Broemme, Dieter; Vieira, Paulo C.; Correa, Arlene G. European Journal of Medicinal Chemistry, 2012 , vol. 54, p. 10 - 21

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Citation Number: 13

Abstract

Cathepsins, also known as lysosomal cysteine peptidases, are members of the papain-like peptidase family, involved in different physiological processes. In addition, cathepsins are implicated in many pathological conditions. This report describes the synthesis and evaluation of a series of N-arylanthranilic acids, acridones, and 4-quinolinones as inhibitors of cathepsins V and L. The kinetics revealed that compounds of the classes of acridones ...