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Synthesis and Antitumor Activity of an Analog of Phthalascidin
引用本文:Ye WANG Yan Li ZHOU Zhan Zhu LIU Shi Zhi CHEN Xiao Guang CHEN. Synthesis and Antitumor Activity of an Analog of Phthalascidin[J]. 中国化学快报, 2006, 17(10): 1279-1282
作者姓名:Ye WANG Yan Li ZHOU Zhan Zhu LIU Shi Zhi CHEN Xiao Guang CHEN
作者单位:Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050
基金项目:国家自然科学基金;北京市自然科学基金
摘    要:Ecteinascidin 743 (Et-743) is an exceedingly potent antitumor agent isolated from the extracts of the marine tunicate Ecteinascidia turbinate1 that is currently undergoing phase Ⅱ/Ⅲ clinical trials in Europe and the United States2. As the result of its …

关 键 词:四氢异喹啉 抗癌抗菌素 Ecteinascidin phthalascidin 合成
收稿时间:2006-04-19

Synthesis and Antitumor Activity of an Analog of Phthalascidin
Ye WANG,Yan Li ZHOU,Zhan Zhu LIU,Shi Zhi CHEN,Xiao Guang CHEN. Synthesis and Antitumor Activity of an Analog of Phthalascidin[J]. Chinese Chemical Letters, 2006, 17(10): 1279-1282
Authors:Ye WANG  Yan Li ZHOU  Zhan Zhu LIU  Shi Zhi CHEN  Xiao Guang CHEN
Abstract:An analog of phthalascidin (Pt-650) was synthesized with an improved synthetic route. With precursor 2 as the starting material, compound 1 was prepared through 4 steps in a total yield of 47%. In vitro antitumor test of this Pt-650 analog showed that it possessed strong toxicity against a number of tumor cell lines including A2780, A549, Bel-7402, BGC-823, HELA, KB, KeTr3 and HCT-8.
Keywords:Ecteinascidin   phthalascidin   tetrahydroisoquinoline   antitumor.
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