Synthesis and structure–activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2, 5-dione structure

…, K Tanaka, B Nicholson, G Deyanat-Yazdi…

文献索引：Yamazaki, Yuri; Tanaka, Koji; Nicholson, Benjamin; Deyanat-Yazdi, Gordafaried; Potts, Barbara; Yoshida, Tomoko; Oda, Akiko; Kitagawa, Takayoshi; Orikasa, Sumie; Kiso, Yoshiaki; Yasui, Hiroyuki; Akamatsu, Miki; Chinen, Takumi; Usui, Takeo; Shinozaki, Yuki; Yakushiji, Fumika; Miller, Brian R.; Neuteboom, Saskia; Palladino, Michael; Kanoh, Kaneo; Lloyd, George Kenneth; Hayashi, Yoshio Journal of Medicinal Chemistry, 2012 , vol. 55, # 3 p. 1056 - 1071

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被引用次数: 38

摘要

Plinabulin (11, NPI-2358) is a potent microtubule-targeting agent derived from the natural diketopiperazine “phenylahistin”(1) with a colchicine-like tubulin depolymerization activity. Compound 11 was recently developed as VDA and is now under phase II clinical trials as an anticancer drug. To develop more potent antimicrotubule and cytotoxic derivatives based on the didehydro-DKP skeleton, we performed further modification on the tert-butyl or phenyl ...