Design, synthesis, and biological evaluation of novel 1-amido-2-one-4-thio-deoxypyranose as potential antitumor agents for multiple myeloma
文献类型：期刊论文
| 作者 | Li, Xiaomei2,3,5; Zhang, Hui4; Dong, Sanfeng3; Gao, Xuejie4; Sun, Haiguo3; Zhou, Zhaoyin3; Hu, Ke4; Guo, Shushan4; Zhang, Qikai4; Guo, Zhufeng1 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2024-09-01 |
| 卷号 | 111页码:16 |
| 关键词 | Multiple myeloma 1-amido-2-one-4-thio-deoxypyranose TRIP13 inhibitor In vivo activity |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2024.117843 |
| 通讯作者 | Xu, Zhijian(zjxu@simm.ac.cn) ; Cai, Haiyan(hanyezi@163.com) ; Shi, Jumei(shijumei@tongji.edu.cn) ; Zhu, Weiliang(wlzhu@simm.ac.cn) |
| 英文摘要 | This study reported the design and synthesis of novel 1-amido-2-one-4-thio-deoxypyranose as inhibitors of potential drug target TRIP13 for developing new mechanism-based therapeutic agents in the treatment of multiple myeloma (MM). In comparison with the positive control DCZ0415, the most active compounds C16, C18, C20 and C32 exhibited strong anti-proliferative activity against human MM cell lines (ARP-1 and NCI-H929) with IC50 values of 1 similar to 2 mu M. While the surface plasmon resonance (SPR) and ATPase activity assays demonstrated that the representative compound C20 is a potent inhibitor of TRIP13, C20 also showed good antitumor activity in vivo on BALB/c nude mice xenografted with MM tumor cells. An initial structure-activity study showed that the carbonyl group is crucial for anticancer activity. Overall, this study provided novel 1-amido-2-one-4-thiodeoxypyranoses, which are entirely different from previously reported potent inhibitor structures of TRIP13, and thus would aid the development of carbohydrate-based novel agents in MM pharmacotherapy. |
| WOS关键词 | MANAGEMENT |
| 资助项目 | National Key Research and Development Program of China[2022YFA1004304] ; National Natural Science Foundation of China[22077131] ; National Natural Science Foundation of China[82170200] ; National Natural Science Foundation of China[82350101] ; National Natural Science Foundation of China[82322067] ; Shanghai Municipal Science and Technology Major Project |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001286214800001 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/312685]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Xu, Zhijian; Cai, Haiyan; Shi, Jumei; Zhu, Weiliang |
| 作者单位 | 1.Shanghai Polytech Univ, Sch Resources & Environm Engn, 2360 Jinhai Rd, Shanghai 201209, 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, Drug Discovery & Design Ctr, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 4.Tongji Univ, Shanghai East Hosp, Dept Hematol, Sch Med, Shanghai 200120, Peoples R China 5.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plants, CAS Lab Chem Plant Resources Arid Reg, Urumqi, Xinjiang, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Xiaomei,Zhang, Hui,Dong, Sanfeng,et al. Design, synthesis, and biological evaluation of novel 1-amido-2-one-4-thio-deoxypyranose as potential antitumor agents for multiple myeloma[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2024,111:16. |
| APA | Li, Xiaomei.,Zhang, Hui.,Dong, Sanfeng.,Gao, Xuejie.,Sun, Haiguo.,...&Zhu, Weiliang.(2024).Design, synthesis, and biological evaluation of novel 1-amido-2-one-4-thio-deoxypyranose as potential antitumor agents for multiple myeloma.BIOORGANIC & MEDICINAL CHEMISTRY,111,16. |
| MLA | Li, Xiaomei,et al."Design, synthesis, and biological evaluation of novel 1-amido-2-one-4-thio-deoxypyranose as potential antitumor agents for multiple myeloma".BIOORGANIC & MEDICINAL CHEMISTRY 111(2024):16. |
入库方式： OAI收割
来源：上海药物研究所
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