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Design, synthesis and biological evaluation of triazolo[1,5-a]pyrimidinone derivatives as potent and orally efficacious WRN helicase inhibitors for MSI cancer therapy

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Microsatellite instability-high (MSI-H) cancers represent an unmet clinical need due to treatment resistance, and WRN helicase is a validated synthetic lethal target for this indication. Herein, we rationally designed, synthesized, and biologically evaluated a... ...