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

被引：11

作者：

Ando, R

Amano, Y

Nakamura, H

Arai, N

Kuwajima, I

机构：

[1] Mitsubishi Pharma Corp, Discovery Technol Lab 2, Aoba Ku, Yokohama, Kanagawa 2270033, Japan

[2] Mitsubishi Pharma Corp, Res Lab 4, Aoba Ku, Yokohama, Kanagawa 2270033, Japan

[3] CREST, Japan Sci & Technol Agcy, Sagamihara, Kanagawa 2288555, Japan

[4] Kitasato Univ, Sagamihara, Kanagawa 2288555, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 12期

关键词：

kazusamycin; antitumor activity;

D O I：

10.1016/j.bmcl.2006.03.056

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (c) 2006 Elsevier Ltd. All rights reserved.

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页码：3315 / 3318

页数：4

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