Synthesis of Hsp90 inhibitor dimers as potential antitumor agents

K Muranaka, A Sano, S Ichikawa, A Matsuda

Index: Muranaka, Kazuhiro; Sano, Akiko; Ichikawa, Satoshi; Matsuda, Akira Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 11 p. 5862 - 5870

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Citation Number: 15

Abstract

Structure-based drug design was used to systematically synthesize PU3-dimers. The cytotoxicity of PU3 dimers 6 against breast cancer cell lines was evaluated, and their potency increased as the length of the bridging linker increased. Among the compounds tested, 6e with a C-20 linker was the most potent and exhibited a 20-to 30-fold increase in activity compared with that of the parent compound 5. Western blot analyses of the cell ...