| First Synthesis of 2a-Thiol Ether Analog of Docetaxel |
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| 作者姓名： | Wei Shuo FANG* Ying LIU Qi Cheng FANG Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing |
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| 作者单位： | Wei Shuo FANG*，Ying LIU，Qi Cheng FANG Institute of Materia Medica，Chinese Academy of Medical Sciences and Peking Union Medical College，Beijing 100050 |
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| 基金项目： | Financial support from Funding to Outstanding Doctor Thesis Authors of Chinese Universities (Grant No. 199949) is gratefully acknowledged by W. S. Fang. |
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| 摘 要： | The chemistry of anticancer drug paclitaxel (=Taxol, 1a) has been extensively explored in recent years. A variety of its analogs with modified taxane frame work or substitutions to its core structure, as well as C-13 substituted isoserine side chains have been synthesized and biologically evaluated1. The marketing of docetaxel (=Taxotere, 1b) is one of the fruitful results from these research efforts. The beginning of clinical trial for analog 2 developed by Indena is the new example. Ba…
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First Synthesis of 2a-Thiol Ether Analog of Docetaxel |
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| Wei Shuo FANG*,Ying LIU,Qi Cheng FANG Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing .First Synthesis of 2a-Thiol Ether Analog of Docetaxel[J].Chinese Chemical Letters,2002(8). |
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| Authors: | Wei Shuo FANG Ying LIU Qi Cheng FANG Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing |
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| Institution: | Wei Shuo FANG*,Ying LIU,Qi Cheng FANG Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050 |
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| Abstract: | A 2a-phenylthio ether analog 1c of docetaxel was synthesized for the first time from 10-deacetylbaccatin III 3 via double inversion of C-2 configuration. This compound showed very weak cytotoxicity toward several tumor cell lines. |
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| Keywords: | Paclitaxel docetaxel thiol ether |
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