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Construction of Diversified Penta-Spiro-Heterocyclic and Fused-Heterocyclic Frameworks with Potent Antitumor Activity

文献类型：期刊论文

作者Liu, Qi1,2; Liu, Xuyi1; Li, Yazhou1; Zhou, Yu1; Zhao, Linxiang2; Liang, Xuewu1; Liu, Hong1,2
刊名CHEMISTRY-A EUROPEAN JOURNAL
出版日期2023-08-14
页码7
关键词spiro fused-heterocyclic frameworks substrate- and pH- controlled strategies C-H activation [4+1] and [4+2] annulation antitumor indazolone
ISSN号0947-6539
DOI10.1002/chem.202301553
通讯作者Liang, Xuewu(liangxuewu0714@simm.ac.cn) ; Liu, Hong(hliu@simm.ac.cn)
英文摘要Multiple-spiro/fused-heterocyclic frameworks containing indazolone are structurally unique and represent a class of potentially dominant skeletons. In this work, we successfully fulfilled Rh(III)-catalyst mediated substrate- and pH- controlled strategies to construct four novel types of complicated penta-spiro/fused-heterocyclic frameworks via C-H activation/[4+1] and [4+2] annulation cascades. This method had mild reaction conditions, a broad scope of substrates, moderate to good yields, and valuable applications, which could realize for the first time the generation of the novel di-spiro-heterocyclic and multiple fused-heterocyclic products with unique structures. More importantly, novel spiro[cyclohexane-indazolo[1,2-a]indazole] scaffold constructed by this method exhibited potent antitumor activity against a variety of refractory solid tumors and hematological malignancies in vitro. Overall, our work provided new insights into the construction of complex and diverse multiple spiro/fused-heterocyclic systems and offered novel valuable lead compounds for the discovery of antitumor drugs.
WOS关键词2-N-SUBSTITUTED INDAZOLONE DERIVATIVES ; 4+2 ANNULATION ; CYCLIZATION ; CINNOLINES
资助项目National Natural Science Foundation of China[21907102] ; National Natural Science Foundation of China[82130105] ; National Natural Science Foundation of China[82173656] ; Lingang Laboratory[LG202103-02-07] ; Lingang Laboratory[LG-QS-202205-09]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:001048010200001
出版者WILEY-V C H VERLAG GMBH
源URL[http://119.78.100.183/handle/2S10ELR8/306956]  
专题新药研究国家重点实验室
通讯作者Liang, Xuewu; Liu, Hong
作者单位1.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China
2.Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Shenyang 110016, Liaoning, Peoples R China
推荐引用方式
GB/T 7714		 Liu, Qi,Liu, Xuyi,Li, Yazhou,et al. Construction of Diversified Penta-Spiro-Heterocyclic and Fused-Heterocyclic Frameworks with Potent Antitumor Activity[J]. CHEMISTRY-A EUROPEAN JOURNAL,2023:7.
APA Liu, Qi.,Liu, Xuyi.,Li, Yazhou.,Zhou, Yu.,Zhao, Linxiang.,...&Liu, Hong.(2023).Construction of Diversified Penta-Spiro-Heterocyclic and Fused-Heterocyclic Frameworks with Potent Antitumor Activity.CHEMISTRY-A EUROPEAN JOURNAL,7.
MLA Liu, Qi,et al."Construction of Diversified Penta-Spiro-Heterocyclic and Fused-Heterocyclic Frameworks with Potent Antitumor Activity".CHEMISTRY-A EUROPEAN JOURNAL (2023):7.

入库方式： OAI收割

来源：上海药物研究所

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