Synthesis, cytotoxicity and antiplasmodial activity of novel ent-kaurane derivatives

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• 作者：Ronan Batista^a ; ^b ; Pablo A. Garcí ; a^c ; Marí ; a Angeles Castro^c ; José ; M. Miguel del Corral^c ; Nivaldo L. Speziali^d ; Fernando de P. Varotti^e ; ^f ; Renata C. de Paula^e ; Luis F. Garcí ; a-Ferná ; ndez^g ; André ; s Francesch^g ; Arturo San Feliciano^c ; Alaí ; de B. de Oliveira^e ; ^{alaide.braga@pq.cnpq.br} ; ^{alaidebraga@terra.com.br}
• 关键词：Wedelia paludosa D.C. ; ent-Kaurane derivatives ; In vitro antimalarial activity ; Plasmodium falciparum ; Antineoplastic activity
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：April, 2013
• 年：2013
• 卷：62
• 期：Complete
• 页码：168-176
• 全文大小：515 K

文摘

This paper reports on the syntheses and spectrometric characterisation of eleven novel ent-kaurane diterpenoids, including a complete set of ¹H, ¹³C NMR and crystallographic data for two novel ent-kaurane diepoxides. Moreover, the antineoplastic cytotoxicity for kaurenoic acid and the majority of ent-kaurane derivatives were assessed in?vitro against a panel of fourteen cancer cell lines, of which allylic alcohols were shown to be the most active compounds. The good in?vitro antimalarial activity and the higher selectivity index values observed for some ent-kaurane epoxides against the chloroquine-resistant W2 clone of Plasmodium falciparum indicate that this class of natural products may provide new hits for the development of antimalarial drugs.