Structure-Guided Design, Synthesis, and Evaluation of Novel 6-Methoxyquinoline-4-carboxamide Derivatives as First-in-Class Nano-Molar B3GAT3 Inhibitors for the Treatment of Hepatocellular Carcinoma
Beta-1,3-glucuronosyltransferase (B3GAT3) is overexpressed in hepatocellular carcinoma (HCC) and correlates with poor prognosis, serving as a desirable anti-HCC target. Based on our micromolar lead TMLB-C16 (IC50 = 6.22−6.53 μM, KD = 3.96 μM), 60 novel derivatives were designed via systematic structure−activity relat...