Synthesis of racemic and optically active forms of novel antimalarial agents, spirocyclopentanone-anthracene adducts, via tandem Michael addition-Dieckmann condensation reactions as the key steps

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• 作者：Ruangrat Choommongkol^a ; Rattana Jongkol^a ; Samran Prabpai^c ; Palangpon Kongsaeree^c ; ^d ; Puttinan Meepowpan^a ; ^b ; ^{pmeepowpan@gmail.com} ; ^{puttinan@chiangmai.ac.th}
• 刊名：Tetrahedron: Asymmetry
• 出版年：2012
• 出版时间：15 March, 2012
• 年：2012
• 卷：23
• 期：5
• 页码：357-363
• 全文大小：789 K

文摘

Spirocyclopentanone-anthracene adducts, novel antimalarial agents, have been synthesized by employing the racemic and the optically active dimethyl itaconate-anthracene adducts in a reaction with piperine via tandem Michael addition-Dieckmann condensation reactions as the key steps. All adducts exhibited antimalarial activity with IC₅₀ values of 3.4-4.7 ¦Ìg/mL, and importantly displayed non-cytotoxicity to vero cells.