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Design, Synthesis, and Biological Evaluation of Naphthoquinone Salts as Anticancer Agents
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Design, Synthesis, and Biological Evaluation of Naphthoquinone Salts as Anticancer Agents
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Journal Article
Design, Synthesis, and Biological Evaluation of Naphthoquinone Salts as Anticancer Agents
2025
Overview
The Warburg effect, a unique glycolytic phenomenon in cancer cells, presents a promising target for developing selective anticancer agents. Previously, BH10, a hit compound disrupting glycolytic metabolism, was identified via phenotypic screening, with Kelch-like ECH-associated protein 1 (Keap1) proposed as a potential target. To enhance its potency and selectivity, a library of BH10-derived salt compounds was synthesized. Among these, 7b exhibited nanomolar anticancer activity (IC50 = 22.97 nM) and a high selectivity ratio (IC50 of non-cancerous cells/IC50 of cancer cells = 41.43). Molecular docking revealed that all naphthoimidazole salt analogues (7a–f) bind to Keap1 via carbonyl-mediated interactions, with variations in hydrogen-bonding residues (e.g., VAL606, ILE559).
Publisher
MDPI AG,MDPI
Subject
/ Analysis
/ Antineoplastic Agents - chemical synthesis
/ Antineoplastic Agents - chemistry
/ Antineoplastic Agents - pharmacology
/ Cancer
/ Cell Proliferation - drug effects
/ Drug Screening Assays, Antitumor
/ Enzymes
/ Glucose
/ Humans
/ Kelch-Like ECH-Associated Protein 1 - chemistry
/ Kelch-Like ECH-Associated Protein 1 - metabolism
/ Molecular Docking Simulation
/ Naphthoquinones - chemical synthesis
/ Naphthoquinones - pharmacology
/ Structure-Activity Relationship
/ Toxicity
