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Synthesis of proline analogues as potent and selective cathepsin S inhibitors |
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| Authors: | Mira Kim Jiyoung Jeon Jiyeon Song Kwee Hyun Suh Young Hoon Kim Kyung Hoon Min Kwang-Ok Lee |
| Affiliation: | 1. Department of Drug Discovery, Hanmi Research Center, 377-1 Yeongcheon-ri, Dongtan-myeon, Hwaseong, Gyeonggi-do 445-813, Republic of Korea;2. College of Pharmacy, Chung-Ang University, Seoul 156-756, Republic of Korea |
| Abstract: | Cathepsin S is a potential target of autoimmune disease. A series of proline derived compounds were synthesized and evaluated as cathepsin S inhibitors. We discovered potent cathepsin S inhibitors through structure–activity relationship studies of proline analogues. In particular, compound 19-(S) showed promising in vitro/vivo pharmacological activities and properties as a selective cathepsin S inhibitor. |
| Keywords: | Cathepsin S Proline analogues Small molecules |
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