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■ Synthesis and Biological Evaluation of NMDI14 Derivatives as Anti-Mesothelioma Agents

Hong Nhung Nguyen, Koya Suzuki, Yasuaki Kimura, Takatsugu Hirokawa, Yuko Murakami-Tonami, and Hiroshi Abe*

*Graduate School of Sceince, Nagoya University, Furo, Chikusa, Nagoya, Aichi 464-8602, Japan

Abstract

Mesothelioma is a severe tumor formed in pleura and peritoneum, for which no useful molecular-targeting therapy is available. We synthesized several derivatives of NMDI14, which is a reported inhibitor for non-sense mediated mRNA decay, and evaluated the activity of the NMDI14 derivatives as potential anti-mesothelioma agents. Some of the synthesized compounds showed promising activity in terms of cytotoxicity toward mesothelioma model cells and promotion of GAS5 expression selectively in mesothelioma cells. These results indicate that the NMDI14 derivatives may be useful for further developing clinically effective anti-mesothelioma drugs.