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23-Oxa-Analogues of OSW-1: Efficient Synthesis and Extremely Potent Antitumor Activity

Authors

  • Bingfeng Shi,

    1. State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Road, Shanghai 200032, P.R. China, Fax: (+86) 21-6416-6128
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  • Hao Wu,

    1. Institute of Biochemistry and Cell Biology, Shanghai Institute for Biological Sciences, Chinese Academy of Sciences, Shanghai 200031, P.R. China
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  • Biao Yu Prof.,

    1. State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Road, Shanghai 200032, P.R. China, Fax: (+86) 21-6416-6128
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  • Jiarui Wu Prof.

    1. Institute of Biochemistry and Cell Biology, Shanghai Institute for Biological Sciences, Chinese Academy of Sciences, Shanghai 200031, P.R. China
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  • This work was supported by the National Natural Science Foundation of China (Grant nos. 20372070, 20321202, and 29925203) and the Chinese Academy of Sciences (Grant no. KGCX2-SW-209).

Abstract

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Eine Aldolkondensation ist der Schlüsselschritt bei der linearen Synthese von 23-Oxa-Analoga des Antitumorwirkstoffs OSW-1. Ausgehend von dem industriell hergestellten Steroid 1 wird 2 in acht Stufen mit über 20 % Gesamtausbeute erhalten. Die Verbindung 2 inhibiert das Wachstum von Tumorzellen bis zu 2000-mal wirksamer als Cisplatin.

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