Preparation of novel ring-A fused azole derivatives of betulin and evaluation of their cytotoxicity

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• 作者：Victoria V. Grishko^a ; ^{grishvic@gmail.com} ; Irina A. Tolmacheva^a ; Vladimir O. Nebogatikov^a ; Natalia V. Galaiko^a ; Alexei V. Nazarov^a ; Maxim V. Dmitriev^b ; Irena B. Ivshina^b ; ^c
• 关键词：Betulin ; Heterocycles ; Azoles ; Tumor cells ; MTT assay ; Apoptosis
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：629-639
• 全文大小：1805 K
• 卷排序：125

文摘

Antitumor activity of the newly synthesized ring-A fused heterocyclic lupane derivatives tested. Structure-activity relationships of new compounds proposed. N-acetyltriazole of betulin with high antiproliferative activity selected. The compound induces early apoptosis in HTC 116 cells by activation of caspases 8 and 3/7.