Synthesis of Succinimide-Containing Chromones, Naphthoquinones, and Xanthones under Rh(III) Catalysis: Evaluation of Anticancer Activity

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• 作者：Sang Hoon Han ; Saegun Kim ; Umasankar De ; Neeraj Kumar Mishra ; Jihye Park ; Satyasheel Sharma ; Jong Hwan KwakSangil Han ; Hyung Sik Kim ; In Su Kim
• 刊名：Journal of Organic Chemistry
• 出版年：2016
• 出版时间：December 16, 2016
• 年：2016
• 卷：81
• 期：24
• 页码：12416-12425
• 全文大小：581K
• ISSN：1520-6904

文摘

The weakly coordinating ketone group directed C–H functionalizations of chromones, 1,4-naphthoquinones, and xanthones with various maleimides under rhodium(III) catalysis are described. These protocols efficiently provide a range of succinimide-containing chromones, naphthoquinones, and xanthones with excellent site selectivity and functional group compatibility. All synthetic compounds were screened for in vitro anticancer activity against human breast adenocarcinoma cell lines (MCF-7). In particular, compounds 7aa and 7ca with a naphthoquinone scaffold were found to be highly cytotoxic, with an activity competitive with anticancer agent doxorubicin.