Hetero-Diels-Alder approach to Bis(indolyl)methanes

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• 作者：Carla Grosso^a ; Ana L. Cardoso^a ; Maria Joã ; o Rodrigues^c ; Cá ; tia Marques^c ; Luí ; sa Barreira^c ; Amé ; rico Lemos^a ; ^b ; Teresa M.D.V. Pinho e Melo^a ; ^{tmelo@ci.uc.pt}
• 关键词：Bis(indolyl)methanes ; Nitrosoalkenes ; Azoalkenes ; Indoles ; Hetero-Diels-Alder reaction ; Anti-cancer activity ; Leukaemia ; Lymphoma
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：1 February 2017
• 年：2017
• 卷：25
• 期：3
• 页码：1122-1131
• 全文大小：1175 K
• 卷排序：25

文摘

A novel synthetic approach to bis(indolyl)methanes has been established. Our one-pot synthetic strategy based on two consecutive hetero-Diels-Alder cycloaddition reactions of electrophilic conjugated nitrosoalkenes with indoles was extended to a range of new 1-hydroxyiminomethyl-bis(indolyl)methanes. Furthermore, a similar and broad range approach was applied to the synthesis of previously unknown 1-hydrazonomethyl-bis(indolyl)methanes. The biological evaluation of the new bis(indolyl)methanes as anti-cancer agents was investigated.