Structure-activity relationships of cyclic enediynes related to dynemicin A—II. Synthesis and antitumor activity of 9-and 12-substituted enediynes equipped with aryl …

…, H Inagaki, Y Suzuki, Y Baba, T Jomori, M Moku…

文献索引：Unno, Ryoichi; Michishita, Hisashi; Inagaki, Hideaki; Suzuki, Yoko; Baba, Yutaka; Jomori, Takahito; Moku, Masatoshi; Nishikawa, Toshio; Isobe, Minoru Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 5 p. 903 - 919

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被引用次数: 19

摘要

Novel enediyne compounds 4–8, simple analogues of dynemicin A (1) equipped with the phenyl or 4-chlorophenyl carbamate moiety, were synthesized and evaluated for DNA- cleaving ability, in vitro cytotoxicity, and in vivo antitumor activity. As a result of the SAR study, it was revealed that the size and character of the substituents (R1 and R2) at the C9 position critically influenced both the stability and antitumor activity of the enediyne ...