"Rhodium-catalysed homo-coupling of terminal alkynes: divergent synthesis of bioactive 1,3-diynes and conjugated enediynes"

作者全名："Xiao, Yijie; Lv, Lijie; Luo, Nanxuan; Zhao, Peirui; Chen, Yao; Luo, Zhangshun; Yin, Houhua; He, Yi; Nie, Shenyou"

作者地址："[Xiao, Yijie; Lv, Lijie; Luo, Nanxuan; Zhao, Peirui; Chen, Yao; Luo, Zhangshun; Yin, Houhua; He, Yi; Nie, Shenyou] Chongqing Med Univ, Affiliated Hosp 2, Inst Life Sci, Basic Med Res & Innovat Ctr Novel Target & Therape, Chongqing 400016, Peoples R China; [Xiao, Yijie; Lv, Lijie; Luo, Nanxuan; Zhao, Peirui; Chen, Yao; Luo, Zhangshun; Yin, Houhua; He, Yi; Nie, Shenyou] Chongqing Med Univ, Affiliated Hosp 2, Dept Urol, Chongqing 400016, Peoples R China; [He, Yi; Nie, Shenyou] Chongqing Med Univ, Coll Pharm, Chongqing 400016, Peoples R China"

通信作者："He, Y; Nie, SY (通讯作者)，Chongqing Med Univ, Affiliated Hosp 2, Inst Life Sci, Basic Med Res & Innovat Ctr Novel Target & Therape, Chongqing 400016, Peoples R China.; He, Y; Nie, SY (通讯作者)，Chongqing Med Univ, Affiliated Hosp 2, Dept Urol, Chongqing 400016, Peoples R China.; He, Y; Nie, SY (通讯作者)，Chongqing Med Univ, Coll Pharm, Chongqing 400016, Peoples R China."

来源：NEW JOURNAL OF CHEMISTRY

ESI学科分类：CHEMISTRY

WOS号：WOS:001196099800001

JCR分区：Q2

影响因子：2.7

年份：2024

卷号：　

期号：　

开始页：　

结束页：　

文献类型：Article; Early Access

关键词：　

摘要："C(sp)-C(sp) cross-coupling of terminal alkynes represents a robust tool for building biologically active 1,3-diynes although confronted with huge challenges regarding selectivity control. Herein, a unique rhodium-catalysed homo-coupling of aromatic terminal alkynes has been achieved, enabling diversity-oriented synthesis (DOS) of 1,3-diynes and conjugated enediynes with high selectivity. Notably, both symmetrical and unsymmetrical 1,3-diynes have been prepared in good yields under mild reaction conditions with wide substrate scope and excellent functional group compatibility. Gratifyingly, further biological evaluation disclosed that the conjugated enediynes exhibited good inhibitory activities against several cancer cell lines. Moreover, 1,3-diyne 2a could effectively inhibit ferroptosis with sub-micromolar activity (EC50 = 114 nM in HT-1080 cell). C(sp)-C(sp) cross-coupling of terminal alkynes represents a robust tool for building biologically active 1,3-diynes although confronted with huge challenges regarding selectivity control."

基金机构：National Natural Science Foundation of China [22177017]; Research foundation of Program for Youth Innovation in Future Medicine from Chongqing Medical University [W0045]; Innovative Group of Natural Science Foundation of Chongqing [CXQT21016]; STI2030-Major Projects [2022ZD0212900]

基金资助正文：The research project was supported by the National Natural Science Foundation of China (22177017); the research foundation of Program for Youth Innovation in Future Medicine from Chongqing Medical University (W0045); and Innovative Group of Natural Science Foundation of Chongqing (CXQT21016) and STI2030-Major Projects (2022ZD0212900).