Synthesis and Anti-tumor Properties of Mono-carbonyl Curcumin Analogues
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摘要: 采用氮烷基化、羟基保护、醛酮缩合三步反应合成了8个新型单羰基姜黄素类似物，结构经质谱、核磁共振氢谱和核磁共振碳谱等手段进行确认。并采用MTT染色法体外检测所合成的8个单羰基姜黄素类似物对人肺癌细胞H1299，结肠癌细胞HT-29，人体胰腺癌细胞BxPC-3和人前列腺癌细胞PC-3的抗癌活性。半数抑制浓度IC50值结果显示：所合成的8个姜黄素类似物对四种细胞均有较强的抑制作用，其中化合物A6在四种细胞中的半数抑制浓度IC50均在0.65 μM以下，抗癌活性比姜黄素提高了40倍以上。
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关键词:
- 抗肿瘤活性
Abstract: Eight Mono-carbonyl curcumin analogues were synthesized by three-step reaction of alkylation, hydroxyl protection, aldehyde ketone condensation. Their structures were characterized by 1H NMR and ESI-MS techniques. Then all the compounds were synthesized and evaluated for their effects on cultured prostate cancer PC-3 cells, pancreas cancer BxPC-3 cells, colon cancer HT-29 cells and lung cancer H1299 cells. These compounds exhibited potent inhibitory effects on the growth of cultured PC-3, BxPC-3, HT-29 and H1299 cells. The IC50 for A6 was lower than 0.65μM in all four cell lines, and A6 was 40-fold more active than curcumin.-
Key words:
- anticancer activity
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