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Late-Stage Functionalization for the Divergent Synthesis of Podophyllotoxin Derivatives by Rhodium Catalysis

文献类型：期刊论文

作者Zhao, Yue1,2; Shen, Yangpeng1,2; He, Jian1,2; Li, Jing2; Zhou, Shengbin3; Wang, Yunbo3; Li, Chunpu2,3; Liu, Hong1,2,3
刊名CHEMISTRY-A EUROPEAN JOURNAL
出版日期2023-05-26
页码10
ISSN号0947-6539
关键词anticancer C-H bond activation divergent synthesis podophyllotoxin late-stage functionalization
DOI10.1002/chem.202300960
通讯作者Li, Chunpu(lichunpu@simm.ac.cn) ; Liu, Hong(hliu@simm.ac.cn)
英文摘要A divergent synthesis of podophyllotoxin derivatives from simple and readily available starting materials through a late-stage functionalization strategy by rhodium catalysis is reported here. This strategy uses the ketone and oxime in substrates as directing groups. Four kinds of novel podophyllotoxin derivatives have been obtained without any erosion of the enantiopurity, thus indicating the broad substrate scope of this method. Additionally, by using the newly developed strategy, 9 aa, which exhibited excellent anticancer activity, can be prepared by a sequential transformation. In particularly, 9 aa suppressed HeLa cells with IC50 values of 74.5 nM, thus providing a promising lead compound for future drug discovery.
WOS关键词TOPOISOMERASE-II ; NATURAL-PRODUCTS ; SELECTIVE FUNCTIONALIZATION ; BIOLOGICAL EVALUATION ; ETOPOSIDE ; ISOQUINOLINE ; INHIBITION ; ANALOGS ; RING
资助项目National Natural Science Foundation of China[82130105] ; National Natural Science Foundation of China[82103969] ; National Natural Science Foundation of China[82273766] ; SA-SIBS Scholarship Program ; Youth Innovation Promotion Association CAS[2020282] ; Lingang Laboratory[LG202103-02-06]
WOS研究方向Chemistry
语种英语
出版者WILEY-V C H VERLAG GMBH
WOS记录号WOS:000995172300001
源URL[http://119.78.100.183/handle/2S10ELR8/306632]  
专题新药研究国家重点实验室
通讯作者Li, Chunpu; Liu, Hong
作者单位1.Nanjing Univ Chinese Med, Sch Chinese Mat Med, 138 Xianlin Ave, Nanjing 210023, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China
3.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Peoples R China
推荐引用方式
GB/T 7714		 Zhao, Yue,Shen, Yangpeng,He, Jian,et al. Late-Stage Functionalization for the Divergent Synthesis of Podophyllotoxin Derivatives by Rhodium Catalysis[J]. CHEMISTRY-A EUROPEAN JOURNAL,2023:10.
APA Zhao, Yue.,Shen, Yangpeng.,He, Jian.,Li, Jing.,Zhou, Shengbin.,...&Liu, Hong.(2023).Late-Stage Functionalization for the Divergent Synthesis of Podophyllotoxin Derivatives by Rhodium Catalysis.CHEMISTRY-A EUROPEAN JOURNAL,10.
MLA Zhao, Yue,et al."Late-Stage Functionalization for the Divergent Synthesis of Podophyllotoxin Derivatives by Rhodium Catalysis".CHEMISTRY-A EUROPEAN JOURNAL (2023):10.

入库方式： OAI收割

来源：上海药物研究所

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