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Discovery and Optimization of Novel TEAD Inhibitors for In Vivo Investigation Against Hepatocellular Carcinoma
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DOI：10.1016/j.ejmech.2026.118886.png)
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Abstract
En 中文
• Cyclization strategy was employed to yield a novel scaffold targeting TEAD palmitate-binding pocket. • Comprehensive and systematic structure-activity relationship (SAR) analysis was conducted. • Optimized compound LC-TD-05 displayed favorable oral bioavailability (F=53.7%). • Compound LC-TD-05 exhibited significant antitumor activity in both in vitro and in vivo HCC models.
Keywords:
TEAD inhibitors
cyclization strategy
hepatocellular carcinoma
structure-activity relationship
oral bioavailability
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5.9
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