Synthesis and structure–activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents

Y Yamazaki, M Sumikura, Y Masuda, Y Hayashi…

文献索引：Hayashi, Yoshio; Yamazaki, Yuri; Sumikura, Makiko; Masuda, Yurika; Hayashi, Yoshiki; Yasui, Hiroyuki; Kiso, Yoshiaki; Chinen, Takumi; Usui, Takeo; Yakushiji, Fumika; Potts, Barbara; Neuteboom, Saskia; Palladino, Michael; Lloyd, George Kenneth Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 14 p. 4279 - 4289

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被引用次数: 18

摘要

KPU-105 (4), a potent anti-microtubule agent that contains a benzophenone was derived from the diketopiperazine-type vascular disrupting agent (VDA) plinabulin 3, which displays colchicine-like tubulin depolymerization activity. To develop derivatives with more potent anti- microtubule and cytotoxic activities, we further modified the benzophenone moiety of 4. Accordingly, we obtained a 4-fluorobenzophenone derivative 16j that inhibited tumor cell ...