A new class of α-ketoamide derivatives with potent anticancer and anti-SARS-CoV-2 activities.

ABSTRACT: Inhibitors of the proteasome have been extensively studied for their applications in the treatment of human diseases such as hematologic malignancies, autoimmune disorders, and viral infections. Many of the proteasome inhibitors reported in the literature target the non-primed site of proteasome's substrate binding pocket. In this study, we designed, synthesized and characterized a series of novel α-keto phenylamide derivatives aimed at both the primed and non-primed sites of the proteasome. In these derivatives, different substituted phenyl groups at the head group targeting the primed site were incorporated in order to investigate their structure-activity relationship and optimize the potency of α-keto phenylamides. In addition, the biological effects of modifications at the cap moiety,

SUBMITTER: Wang J 

PROVIDER: S-EPMC7873610 | biostudies-literature | 2021 Apr

REPOSITORIES: biostudies-literature