Synthesis and biological evaluation of pyrazole-fused oleanolic acid derivatives as novel inhibitors of inflammatory and osteoclast differentiation
文献类型：期刊论文
| 作者 | Yu, Yuanyuan4,5; Yuan, Wenlong2,3; Yuan, Jiaqi2,4; Wei, Wenhui2,3; He, Qian4 ; Zhang, Xiaofei4; He, Shijun1,2,3; Yang, Chunhao1,2,4,5
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
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| 出版日期 | 2023-02-15 |
| 卷号 | 80页码:117177 |
| 关键词 | Osteoarthritis Oleanolic acid derivatives Anti-inflammatory IL-1? inhibition Antiosteoclastic activity |
| DOI | 10.1016/j.bmc.2023.117177 |
| 文献子类 | Article |
| 英文摘要 | A series of pyrazole-fused oleanolic acid derivatives were designed and synthesized. The modification of these analogues focused on the substituents screening on the pyrazole ring. The cytotoxicity of these compounds and their anti-inflammatory activities via inhibiting interleukin-1 beta (IL-1 beta) production were evaluated in RAW264.7 cells. Most of the derivatives showed significantly improved potency compared with oleanolic acid. Among them, compound 7n exhibited the most potent anti-inflammatory activity on decreasing IL-1 beta production with low cytotoxicity. Moreover, the further study found 7n could inhibit RANKL-induced osteoclast differentiation on bone marrow-derived macrophages (BMMs). These findings may provide a potential direction for the drug development of osteoarthritis. |
| WOS关键词 | OSTEOARTHRITIS ; ANTIOXIDANT ; KNEE ; HIP |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000960753500001 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/309717]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | He, Shijun; Yang, Chunhao |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, Sch Pharm, 19A Yuquan Rd, Beijing 100049, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Lab Immunopharmacol, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China; 4.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, State Key Lab Drug Res, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China; 5.Nanjing Univ Chinese Med, Sch Chinese Mat Med, 138 Xianlin Ave, Nanjing 210023, Jiangsu, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Yu, Yuanyuan,Yuan, Wenlong,Yuan, Jiaqi,et al. Synthesis and biological evaluation of pyrazole-fused oleanolic acid derivatives as novel inhibitors of inflammatory and osteoclast differentiation[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2023,80:117177. |
| APA | Yu, Yuanyuan.,Yuan, Wenlong.,Yuan, Jiaqi.,Wei, Wenhui.,He, Qian.,...&Yang, Chunhao.(2023).Synthesis and biological evaluation of pyrazole-fused oleanolic acid derivatives as novel inhibitors of inflammatory and osteoclast differentiation.BIOORGANIC & MEDICINAL CHEMISTRY,80,117177. |
| MLA | Yu, Yuanyuan,et al."Synthesis and biological evaluation of pyrazole-fused oleanolic acid derivatives as novel inhibitors of inflammatory and osteoclast differentiation".BIOORGANIC & MEDICINAL CHEMISTRY 80(2023):117177. |
入库方式： OAI收割
来源：上海药物研究所
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