期刊
ORGANIC CHEMISTRY FRONTIERS
卷 8, 期 8, 页码 1808-1816出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/d1qo00134e
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资金
- National Natural Science Foundation of China [21971262, 81702255]
- National Postdoctoral Program for Innovative Talents [BX20190399]
- Guangdong Provincial Key Laboratory of Chiral Molecule and Drug Discovery [2019B030301005]
- Program for Guangdong Introducing Innovative and Entrepreneurial Teams [2016ZT06Y337]
A new synthesis method for 2-indolyl indolone N-oxides via gold(i)-catalyzed cascade reaction of o-nitroalkynes with indoles has been developed, leading to highly efficient conversion into 2-indolylbenzoxazinone with strong blue fluorescence. The synthesized compounds were also evaluated for their antitumor activity in small cell lung cancer, with compounds 3d and 4s showing high anticancer potency against SCLC cells.
An efficient and practical method for the synthesis of 2-indolyl indolone N-oxides via gold(i)-catalyzed cascade reaction of o-nitroalkynes with indoles has been reported. The generated product could be readily converted into the 2-indolylbenzoxazinone, which emits strong blue fluorescence. We also investigated the antitumor activity of these synthesized compounds in small cell lung cancer (SCLC), and the results show that compounds 3d and 4s exhibit high anticancer potency against SCLC cells.
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