The Preparation and Evaluation of 1-Substituted 1,2,3,4-Tetrahydro- and 3,4-Dihydro-β-carboline Derivatives as Potential Antitumor Agents

Shen Ya-Ching, Chen Ching-Yeu, Hsieh Pei-Wen, Duh Chang-Yih, Lin Yat-Min, Ko Chin-Lien

doi:10.1248/cpb.53.32

The Preparation and Evaluation of 1-Substituted 1,2,3,4-Tetrahydro- and 3,4-Dihydro-β-carboline Derivatives as Potential Antitumor Agents

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Shen Ya-Ching

Institute of Marine Resources, National Sun Yat-sen University, Taiwan
Chen Ching-Yeu

Institute of Marine Resources, National Sun Yat-sen University, Taiwan
Hsieh Pei-Wen

Institute of Marine Resources, National Sun Yat-sen University, Taiwan
Duh Chang-Yih

Institute of Marine Resources, National Sun Yat-sen University, Taiwan
Lin Yat-Min

Institute of Marine Resources, National Sun Yat-sen University, Taiwan
Ko Chin-Lien

Institute of Marine Resources, National Sun Yat-sen University, Taiwan

書誌事項

タイトル別名

The Preparation and Evaluation of 1-Substituted 1,2,3,4-Tetrahydro- and 3,4-Dihydro-.BETA.-carboline Derivatives as Potential Antitumor Agents
Preparation and Evaluation of 1 Substituted 1 2 3 4 Tetrahydro and 3 4 Dihydro ベータ carboline Derivatives as Potential Antitumor Agents

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説明

A series of 1-substituted 1,2,3,4-tetrahydro- and 3,4-dihydro-β-carboline derivatives have been synthesized and evaluated for antitumor activity against murine P-388 and human tumor cell lines, KB-16, A-549 and HT-29. All of the compounds prepared, except for 19, showed significant cytotoxicity. Among them, compound 29 exhibited the most potent activity against all tested tumor cell lines. There was an apparent lack of correlation regarding cytotoxicity between 1,2,3,4-tetrahydro- and 3,4-dihydro-β-carbolines. This study is the first to discover compound 29 as a potential lead for the development of future anticancer agents. The mode of inhibition for compound 29 was proposed.