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Bifunctional chimeric heterocyclic compound and use thereof as androgen receptor degrader

PendingEP4378936A4effectively inhibit the proliferation of drug-resistant prostate cancer cellsmaintain good propertiesOrganic chemistryAntiviralsAndrogen Receptor GeneBifunctional
A compound as shown in formula I, or an optical isomer thereof, a solvate thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, a tautomer thereof, a mesomer thereof, a racemate thereof, an enantiomer thereof, a diastereomer thereof, a mixture form thereof, a metabolite thereof, a metabolic precursor thereof, or an isotope substitute form thereof. TB is a target recognition / binding portion, L is a linking portion, and U is a ubiquitin protease recognition / binding portion, the three portions being connected by means of chemical bonds. The compound can significantly down-regulate mutated androgen receptor (AR) proteins, and has good inhibitory activity on prostate cancer cell lines. The compound of formula I can be used for preparation of a protein degradation targeted chimera for targeted regulation of androgen receptors, and a drug for treating diseases correlated with regulation by androgen receptors, and has particularly good application prospects in drugs for treating prostate cancers and breast cancers.
Owner:HINOVA PHARM INC