Synthesis and antitumor activity of the estrane analogue of OSW-1

Synthesis and antitumor activity of the estrane analogue of OSW-1
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DOI:
10.1002/ejoc.200400632
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发表时间:
2005-03
影响因子:
2.8
通讯作者:
Y. Matsuya;Seiji Masuda;N. Ohsawa;S. Adam;T. Tschamber;J. Eustache;K. Kamoshita;Y. Sukenaga;H. Nemoto*
Y. Matsuya;Seiji Masuda;N. Ohsawa;S. Adam;T. Tschamber;J. Eustache;K. Kamoshita;Y. Sukenaga;H. Nemoto*
中科院分区:
化学3区
文献类型:
--
作者:
Y. Matsuya;Seiji Masuda;N. Ohsawa;S. Adam;T. Tschamber;J. Eustache;K. Kamoshita;Y. Sukenaga;H. Nemoto*

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以雌酮为起始原料,经12步反应合成了具有抗肿瘤活性的天然皂苷OSW-1的雌甾烷类似物。研究了该化合物对几种人恶性肿瘤细胞的细胞抑制活性,并与天然OSW-1和顺铂的细胞抑制活性进行了比较,结果表明,甾体成分的修饰可能是寻找新的抗癌药物候选物的有效途径。(© Wiley-VCH Verlag GmbH & Co. KGaA,69451魏因海姆,德国,2005)
The estrane analogue of OSW-1, a potent antitumor natural saponin, was efficiently synthesized from estrone in 12 steps. The cytostatic activity of the compound against several human malignant tumor cells was examined and compared to those of the natural OSW-1 and cisplatin, the results suggesting that the modification of the steroidal component could be an effective approach in the search for new candidates of anticancer drugs. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005)