Title of article :
Synthesis and structure–activity relationships of 3-substituted 1,4-dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridines as novel antitumor agents
Author/Authors :
Yasunori Tsuzuki، نويسنده , , Kyoji Tomita، نويسنده , , Yuji Sato and Hiromitsu Ishii، نويسنده , , Shigeki Kashimoto، نويسنده , , Katsumi Chiba، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2004
Pages :
5
From page :
3189
To page :
3193
Abstract :
In order to obtain clinically useful antitumor agent, we have designed and synthesized various 3-substituted 1,4-dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridines, and evaluated their cytotoxic activity. The series of novel 3-substituted derivatives synthesized in this study showed good antitumor activity against murine P388 leukemia. Particularly, the 3-formyl 1,8-naphthyridine displayed an antitumor activity equal to that of the 3-carboxy 1,8-naphthyridine against murine and human tumor cell lines as well as in vivo test for mouse leukemia. These results demonstrate that the carboxy group at the C-3 position of 1,8-naphthyridine ring is not essential for antitumor activity. In addition, the trend of cytotoxic activity for the 3-substituted 1,8-naphthyridines was different from that of antibacterial activity.
Journal title :
Bioorganic & Medicinal Chemistry Letters
Serial Year :
2004
Journal title :
Bioorganic & Medicinal Chemistry Letters
Record number :
794563
Link To Document :
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