10-羟基氮杂solamin类似物的合成及其生物活性  

Synthesis and biological activity of 10-hydroxylated aza-solamin

作　　者：王猛[1] 唐卫东[1] 楼丽广[1] 王昕[1] 沈竞康[1] 

机构地区：[1]中国科学院上海药物研究所新药研究国家重点实验室,上海201203

出　　处：《中国药物化学杂志》2006年第4期214-217,共4页Chinese Journal of Medicinal Chemistry

摘　　要：目的设计合成新型番荔枝内酯氮杂类似物,评价其抗肿瘤活性。方法以氮杂solamin为分子模型,运用生物电子等排原理,设计并合成10-羟基氮杂solamin类似物,并与前体化合物比较对HL-60、LoVo和HT-29肿瘤细胞株的生长抑制作用。结果该化合物未见文献报道,其结构经IR1、H-NMR及MS确证。结论所设计的氮杂类似物具有一定程度的抗肿瘤活性,羟基官能团对化合物抗肿瘤活性具有一定贡献。Aim A novel aza-acetogenin analogue was designed and synthesized to study its antitumor activity. Methods Based on the aza-solamin molecular template, 10-hydroxyl aza-solamin was synthesized through multi-step chemical reactions. The antitumor activities of the 10-hydroxyl analogue, along with the precursor compounds, was assessed by inhibiting HL-60, LoVo and HT-29 tumor cells growth in vitro using MTT method. Results The 10-hydroxylated aza-solamin was first synthesized successfully, and its structure was confirmed by IR, ^1H-NMR and MS specta. Conclusion The preliminary tests in vitro show that these novel solamin analogues still retain certain antitumor activities, and the polar functional group at alkyl spacer of the moiety would benefit its activity against some tumor cells.

关 键 词：药物化学 化合物制备 化学合成 氮杂solamin类似物 番荔枝内酯 抗肿瘤 

分 类 号：R914[医药卫生—药物化学]