pevonedistat has been researched along with Colonic-Neoplasms* in 1 studies
1 other study(ies) available for pevonedistat and Colonic-Neoplasms
Article | Year |
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Discovery of benzothiazole derivatives as novel non-sulfamide NEDD8 activating enzyme inhibitors by target-based virtual screening.
NEDD8 activating enzyme (NAE) plays a critical role in various cellular functions in cancers. In this study, a target-based virtual screening was applied to discover benzothiazoles to be potent non-covalent NAE inhibitors. Further two round optimizations concluded a preliminary structure-activity relationship (SAR) of their derivatives. Three compounds (6k, 7b, ZM223) exhibited antitumor activities in nanomolar range. ZM223 showed excellent anticancer activity against HCT116 colon cancer cells with an IC Topics: Antineoplastic Agents; Benzothiazoles; Cell Line, Tumor; Colonic Neoplasms; Enzyme Inhibitors; HCT116 Cells; Humans; Models, Molecular; Structure-Activity Relationship; Ubiquitin-Activating Enzymes | 2017 |