Design,synthesis and biological evaluation of novel HIV-1 protease inhibitors with pentacyclic triterpenoids as P2-ligands |
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| Authors: | Mei Zhu Xiao-Nan Du Yun-Ge Li Guo-Ning Zhang Ju-Xian Wang Yu-Cheng Wang |
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| Affiliation: | 1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, China;2. School of Pharmacy, Jinzhou Medical University, Jinzhou, Liaoning 121001, China |
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| Abstract: | The design, synthesis and SAR study of a new series of HIV-1 protease inhibitors with pentacyclic triterpenoids as P2 ligands and phenylsulfonamide as P2′ ligands were discussed. These compounds exhibited micromolar inhibitory potency, among which compound T1c displayed HIV-1 protease inhibition with IC50 values of 0.12?μM, which was 67 times the inhibitory activity of its raw material Ursolic acid (8.0?μM). |
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| Keywords: | HIV-1 protease inhibitors P2 ligand Pentacyclic triterpenoids |
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