Potent antitumor activity of synthetic 1,2-naphthoquinones and 1,4-naphthoquinones
Potent antitumor activity of synthetic 1,2-naphthoquinones and 1,4-naphthoquinones
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DOI：
10.1016/s0968-0896(03)00226-8
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发表时间：
2003-07-17
影响因子：
3.5
通讯作者：
Kongsaeree, P
中科院分区：
文献类型：
--
作者：
Kongkathip, N;Kongkathip, B;Kongsaeree, P
合成了Rhinacanthone（1）和两个1，2-吡喃萘醌（2，3），发现它们对三种癌细胞系（KB、HeLa和HepG（2））显示出非常强的细胞毒性，IC 50值为0.92-9.63 μ M，而相应的羟基化衍生物4具有降低的细胞毒性（IC 50值为7.61-24.13 μ M）。还合成了三个1，2-呋喃并萘醌衍生物（5-7），它们具有与1，2-吡喃并萘醌类似的细胞毒性。与1，2-萘醌类化合物相比，合成了6个含吡喃环（8-10）和呋喃环（11-13）的n-1，4-萘醌类化合物，它们对肿瘤细胞的细胞毒性较小或无活性。此外，化合物13对HeLa细胞系具有显著的细胞毒性（IC 50值为9.25 μ M），而对vero细胞没有毒性。(C)2003爱思唯尔科技有限公司版权所有。
Rhinacanthone (1) and two 1,2-pyranonaphthoquinones (2,3) were synthesized and found to show very potent cytotoxicity against three cancer cell lines (KB, HeLa and HepG(2)) with IC50 values of 0.92-9.63 muM, whereas the corresponding hydroxylated derivative 4 had reduced cytotoxicity (IC50 values of 7.61-24.13 muM). Three 1,2-furanonaphthoquinone derivatives (5-7) were also synthesized with similar cytotoxicity as 1,2-pyranonaphthoquinones. In comparison to 1,2-naphthoquinones, six w1,4-naphthoquinones derivatives fused with pyran ring (8-10) and furan ring (11-13) were synthesized and they showed less cytotoxicity or inactive to the cancer cell lines. Moreover, compound 13 had significant cytotoxicity against HeLa cell line (IC50 value of 9.25 muM) while it showed no toxic to vero cell. (C) 2003 Elsevier Science Ltd. All rights reserved.