Mitochondrial-targeting devimistat derivatives, methods of making and using the same
By conjugating a mitochondrial-targeting derivative with the TPP group to Devimistat, the problem of insufficient accumulation of Devimistat in mitochondria was solved, achieving highly efficient inhibition of proliferation and induction of apoptosis in tongue squamous cell carcinoma cells, significantly reducing the IC50 value, improving the chemical structural stability, and making it suitable for anti-tumor drugs.
CN122277608APending Publication Date: 2026-06-26YUYAO PEOPLES HOSPITAL
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Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- YUYAO PEOPLES HOSPITAL
- Filing Date
- 2026-03-31
- Publication Date
- 2026-06-26
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Figure CN122277608A_ABST
Abstract
This invention relates to the field of pharmaceutical chemistry, specifically to a Devimistat derivative with mitochondrial targeting function, its preparation method, and its application in antitumor drugs. This derivative covalently couples the mitochondrial-attractant 3-aminopropyl(triphenyl)phosphine bromide (TPP) group to the antitumor active molecule Devimistat, utilizing the affinity of the TPP cation for the mitochondrial transmembrane potential to drive the drug's specific accumulation in the mitochondrial matrix. While retaining the original drug's interference with the tricarboxylic acid cycle and inhibition of PDH and KGDH complex activity, this derivative significantly increases the effective drug concentration within tumor cells, thus solving the problem of limited efficacy of Devimistat due to its lack of targeting.
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