| Autor: |
Chen, Chao, Yu, Wenwen, Huang, Guangen, Ren, Xuelian, Chen, Xiangli, Li, Yixin, Liang, Shenggui, Xu, Mengmeng, Zheng, Mingyue, Yang, Yaxi, Huang, He, Tang, Wei, Zhou, Bing |
| Zdroj: |
Chinese Chemical Letters; November 2024, Vol. 35 Issue: 11 |
| Abstrakt: |
The development of enantioselective CH macrocyclizations to efficiently access structurally diversified macrocycles is highly desirable, but remain a big challenge. Herein, we reported the first rhodium(III)-catalyzed asymmetric intramolecular CH macrocyclization, enabling the efficient synthesis of structurally diverse enantioenriched macrocycles. This robust enantioselective CH macrocyclization has a broad functional group tolerance, excellent enantioselectivities (up to 98.5:1.5 e.r.) and a mild reaction condition, releasing CO2as the single by-product. More significantly, the resulting unique enantioenriched 19-membered macrocycle 2fwas found to demonstrate a potent in vitroanti-Zika virus (ZIKV) activity without obvious cytotoxicity. Further investigation revealed that the anti-ZIKV activity is presumably attributed to an autophagy inhibition in the early stage of viral infection by down-regulating the expression of autophagy related gene Atg12. |
| Databáze: |
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