Design, synthesis and biological evaluation of 4-amino substituted 2H-chromen-2-one derivatives as an NEDD8 activating enzyme inhibitor in pancreatic cancer cells.

CONCLUSION: Based on these results, we found that compound 21 inhibited NAE activity in an ATP-dependent manner in enzyme-based system, induced apoptosis in BxPC-3 cells and synergized with bortezomib on BxPC-3 cell growth inhibition. Additionally, it had low toxicity with reasonable Log P value and water solubility. PMID: 31880252 [PubMed - as supplied by publisher]
Source: Medicinal Chemistry - Category: Chemistry Authors: Tags: Med Chem Source Type: research