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Communication | Special issue | Vol 95, No. 1, 2017, pp.181-186
Published online, 1st February, 2017
DOI: 10.3987/COM-16-S(S)51
Design and Synthesis of 4-Chlorocolchicine-Derived Prodrug Capable of Forming Nanoparticles by Self-Assembly

Mariko Kitajima, Akihiro Morita, Shimpei Endo, Noriyuki Kogure, Kenjirou Higashi, Kunikazu Moribe, and Hiromitsu Takayama*

*Laboratory of Biofunctional Molecular Chemistry, Graduate School of Pharmaceutical Sciences, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan


We have designed and synthesized colchicine-derived prodrug 7, which is composed of a 4-chlorocolchicine derivative, a dipeptide side chain cleavable by cathepsin B, a spacer containing a disulfide bond, and hydrophobic vitamin E. Prodrug 7 was capable of forming nanoparticles by self-assembly. Mean particle diameter evaluated by dynamic light scattering measurement was ca. 205 nm.