Design, synthesis, and STING-agonistic activity of benzo[b]thiophene-2-carboxamide derivatives
文献类型：期刊论文
| 作者 | Zhou, Rongyao3,4; Wang, Xiyuan2; Zhang, Deqiang2; Zhan, Zhengsheng1,3,4; Duan, Wenhu1,3,4
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| 刊名 | MOLECULAR DIVERSITY
 |
| 出版日期 | 2023-10-05 |
| 页码 | 10 |
| 关键词 | STING CDN Benzo[b]thiophene-2-carboxamide Cellular activity |
| ISSN号 | 1381-1991 |
| DOI | 10.1007/s11030-023-10736-1 |
| 通讯作者 | Zhan, Zhengsheng(zszhan@simm.ac.cn) ; Duan, Wenhu(whduan@simm.ac.cn) |
| 英文摘要 | STING is an important immune-associated protein that localizes in the endoplasmic reticulum membrane. Upon being activated by its agonists, STING triggers the IRF and NF-kappa B pathways, which generates type I interferons and proinflammatory cytokines, and ultimately primes the innate immune responses to achieve valid antitumor efficacy. We designed and synthesized a series of benzo[b]thiophene-2-carboxamide derivatives. Through STING-agonistic activity evaluation, compounds 12d and 12e exhibited marginal human STING-activating activities. Western blot analysis demonstrated that both 12d and 12e treatment increased the phosphorylation of the downstream signaling molecules (TBK1 and IRF3) of STING. The proposed binding mode of 12d/12e and STING protein displayed that two canonical hydrogen bonds, a pi-pi stacking interaction, as well as a pi-cation interaction formed between the agonist and the CDN-binding domain of STING protein. |
| WOS关键词 | C-DI-GMP ; I INTERFERON ; AMP ; ACTIVATION ; CELLS ; TUMOR |
| 资助项目 | We thank Shanghai Institute of Materia Medica (no. CASIMM0120215010), the Lingang Laboratory (No. LG202103-02-08), Science and Technology Commission of Shanghai Municipality (No. 21ZR1475700) for their financial support.[CASIMM0120215010] ; Shanghai Institute of Materia Medica[LG202103-02-08] ; Lingang Laboratory[21ZR1475700] ; Science and Technology Commission of Shanghai Municipality |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001078735900001 |
| 出版者 | SPRINGER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/307303]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Zhan, Zhengsheng; Duan, Wenhu |
| 作者单位 | 1.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Materia Med, Div Antitumor Pharmacol, State Key Lab Drug Res, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Materia Med, Small Mol Drug Res Ctr, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China 4.Nanjing Univ Chinese Med, Sch Chinese Materia Med, Nanjing 210023, Jiangsu, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhou, Rongyao,Wang, Xiyuan,Zhang, Deqiang,et al. Design, synthesis, and STING-agonistic activity of benzo[b]thiophene-2-carboxamide derivatives[J]. MOLECULAR DIVERSITY,2023:10. |
| APA | Zhou, Rongyao,Wang, Xiyuan,Zhang, Deqiang,Zhan, Zhengsheng,&Duan, Wenhu.(2023).Design, synthesis, and STING-agonistic activity of benzo[b]thiophene-2-carboxamide derivatives.MOLECULAR DIVERSITY,10. |
| MLA | Zhou, Rongyao,et al."Design, synthesis, and STING-agonistic activity of benzo[b]thiophene-2-carboxamide derivatives".MOLECULAR DIVERSITY (2023):10. |
入库方式： OAI收割
来源：上海药物研究所
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