Ontology highlight
ABSTRACT:
SUBMITTER: Lawrence HR
PROVIDER: S-EPMC3530924 | biostudies-literature | 2010 Aug
REPOSITORIES: biostudies-literature
Lawrence Harshani R HR Kazi Aslamuzzaman A Luo Yunting Y Kendig Robert R Ge Yiyu Y Jain Sanjula S Daniel Kenyon K Santiago Daniel D Guida Wayne C WC Sebti Saïd M SM
Bioorganic & medicinal chemistry 20100618 15
Screening of the NCI Diversity Set-1 identified PI-083 (NSC-45382) a proteasome inhibitor selective for cancer over normal cells. Focused libraries of novel compounds based on PI-083 chloronaphthoquinone and sulfonamide moieties were synthesized to gain a better understanding of the structure-activity relationship responsible for chymotrypsin-like proteasome inhibitory activity. This led to the demonstration that the chloronaphthoquinone and the sulfonamide moieties are critical for inhibitory a ...[more]