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. 2006 Jun 15;16(12):3315-8.
doi: 10.1016/j.bmcl.2006.03.056. Epub 2006 Apr 17.

Design, synthesis, and evaluation of novel kazusamycin A derivatives as potent antitumor agents

Ryoichi Ando  1 , Yusaku Amano, Hideo Nakamura, Noriyoshi Arai, Isao Kuwajima
Affiliations

Design, synthesis, and evaluation of novel kazusamycin A derivatives as potent antitumor agents

Ryoichi Ando et al. Bioorg Med Chem Lett. .

Abstract

Novel kazusamycin A derivatives were designed in the viewpoint of decrease of reactivity at the alpha,beta-unsaturated delta-lactone moiety against Michael-type addition. Although 25-30 steps were required for the synthesis of each compound, their syntheses were achieved. Cytotoxicity against HPAC cell line was evaluated, and two of them exhibited comparable potency to kazusamycin A. Hepatic toxicity of these designed compounds was much lower than that of kazusamycin A.

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