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- Ga-Yeong Kim, Chae Won Song, Yo-Sep Yang, Na-Rae Lee, Hyung-Seok Yoo, Seung Hwan Son, Soo Jin Lee, Jong Seon Park, Jong Kil Lee, Kyung-Soo Inn, and Nam-Jung Kim.
- College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Dongdaemun-gu, Seoul 02447, Korea.
- Molecules. 2021 Apr 26; 26 (9).
AbstractA series of PROTACs (PROteolysis-TArgeting Chimeras) consisting of bicalutamide analogs and thalidomides were designed, synthesized, and biologically evaluated as novel androgen receptor (AR) degraders. In particular, we found that PROTAC compound 13b could successfully demonstrate a targeted degradation of AR in AR-positive cancer cells and might be a useful chemical probe for the investigation of AR-dependent cancer cells, as well as a potential therapeutic candidate for prostate cancers.
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