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Development of a Series of Tanshinone Derivatives Through Scaffold Hopping for Treating Non-Small-Cell Lung Cancer (NSCLC)

文献类型：期刊论文

作者Zhou, Lan-Xin3,4; Shu, Zheng-Yu3; Li, Heng2; Zhong, Hui4,5; Xu, Dou-Nan4; Tang, Lei1,3; Hu, Chu-Jiao1,3; Luo, Cheng1,2,3,4,5; Xiong, Huan4
刊名MOLECULES
出版日期2026-01-27
卷号31期号:3页码:27
关键词tanshinone derivatives scaffold hopping NSCLC cytotoxic activity
DOI10.3390/molecules31030446
通讯作者Hu, Chu-Jiao(huchujiao2021@gmc.edu.cn) ; Luo, Cheng(luocheng@zidd.ac.cn) ; Xiong, Huan(xionghuan@zidd.ac.cn)
英文摘要Non-small-cell lung cancer (NSCLC) is one of the most prevalent cancer types and accounts for the majority of cancer-related deaths worldwide. Tanshinone and its derivatives exhibit diverse biological activities, and their prominent antitumor potential has been well documented. In this study, we rationally designed a series of tanshinone derivatives with a scaffold-hopping strategy. Thirty-five tanshinone derivatives were synthesized, and their cytotoxic activities against the NSCLC cell lines A549 and H838 were investigated. Concurrently, their safety profile was assessed in BEAS-2B cells. The results showed that compounds S2-1, S2-4, and S2-8 exhibited superior inhibitory activity against A549 cells compared with the positive control, beta-lapachone. Meanwhile, compounds S2-1, S2-3, S2-4, S2-8, S2-13, and S2-14 exhibited similar or increased antiproliferation activity against H838 cells. Compounds S2-4 (0.58 +/- 0.07 mu M) and S2-8 (0.42 +/- 0.04 mu M) demonstrated the greatest potency towards H838 cells; compounds S2-13 (1.28 +/- 0.13 mu M) and S2-14 (1.80 +/- 0.24 mu M) exhibited potent and selective activity towards H838 cells. Molecular docking studies of S2-4/NLRP3 and S2-14/STAT3, combined with the structure-activity relationship (SAR) analysis, indicated that the benzofuran core containing an ortho-quinone, along with an amide linkage and a 1,2,3-triazole group introduced at the C-2 position of the furan ring, is an effective chemical scaffold for enhancing the anti-NSCLC activity of tanshinone derivatives.
WOS关键词INHIBITORS ; ANALOGS
资助项目Science and Technology Department of Guizhou Province[[2024]015] ; Science and Technology Department of Guizhou Province[[2026(341)]]
WOS研究方向Biochemistry & Molecular Biology ; Chemistry
语种英语
WOS记录号WOS:001687944900001
出版者MDPI
源URL[http://119.78.100.183/handle/2S10ELR8/322966]  
专题中国科学院上海药物研究所
通讯作者Hu, Chu-Jiao; Luo, Cheng; Xiong, Huan
作者单位1.Key Lab Canc Prevent & Treatment Guizhou Prov, Guiyang 550004, Peoples R China
2.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China
3.Guizhou Med Univ, State Key Lab Discovery & Utilizat Funct Component, Guizhou Prov Key Lab Innovat & Mfg Pharmaceut, Guiyang 550004, Peoples R China
4.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Shanghai Inst Mat Med, Zhongshan 528400, Peoples R China
5.Guangzhou Univ Chinese Med, Guangzhou 510006, Peoples R China
推荐引用方式
GB/T 7714		 Zhou, Lan-Xin,Shu, Zheng-Yu,Li, Heng,et al. Development of a Series of Tanshinone Derivatives Through Scaffold Hopping for Treating Non-Small-Cell Lung Cancer (NSCLC)[J]. MOLECULES,2026,31(3):27.
APA Zhou, Lan-Xin.,Shu, Zheng-Yu.,Li, Heng.,Zhong, Hui.,Xu, Dou-Nan.,...&Xiong, Huan.(2026).Development of a Series of Tanshinone Derivatives Through Scaffold Hopping for Treating Non-Small-Cell Lung Cancer (NSCLC).MOLECULES,31(3),27.
MLA Zhou, Lan-Xin,et al."Development of a Series of Tanshinone Derivatives Through Scaffold Hopping for Treating Non-Small-Cell Lung Cancer (NSCLC)".MOLECULES 31.3(2026):27.

入库方式： OAI收割

来源：上海药物研究所

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