Synthesis and antitumor activity of novel α-aminophosphonates from diterpenic dehydroabietylamine
Synthesis and antitumor activity of novel α-aminophosphonates from diterpenic dehydroabietylamine
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DOI：
10.1002/hc.20471
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发表时间：
2008-01-01
影响因子：
0.3
通讯作者：
He, Ling
中科院分区：
文献类型：
--
作者：
Rao, Xiaoping;Song, Zhanqian;He, Ling
以脱氢松香胺为原料合成了一系列新型α-氨基膦酸酯类化合物，其结构经红外光谱、核磁共振氢谱和核磁共振波谱确证。用四甲基偶氮唑盐比色法测定其对SMMC7721肝癌细胞的抑瘤活性。化合物4和6在极低浓度下仍表现出较高的抑制率，当浓度为0时，抑制率分别达到75%和79%。1亩M。化合物9孵育72 h后，抑制率达99%。具有氟原子和与苯环相连的硝基的氨基膦酸酯具有较高的活性。(C)2008年威利期刊公司。
A series of novel a-aminophosphonates were synthesized from diterpenic dehydroabietylamine, and their structures were characterized by IR, H-1 NMR, and P-31 NMR spectroscopy. Their antitumor activities against SMMC7721 liver cancer cells were evaluated by the MTT method. Compounds 4 and 6 exhibited higher activities even at vety low concentrations, and the inhibition ratios reached 75% and 79% at 0. 1 mu M, respectively. The inhibition ratio of compound 9 reached 99% after 72-h incubation. aAminophosphonates with a fluorine atom and a nitro group fused to the benzene ring exhibited higher activities. (c) 2008 Wiley Periodicals, Inc.