The Preparation and Evaluation of 1-Substituted 1,2,3,4-Tetrahydro- and 3,4-Dihydro-.BETA.-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

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  • The Preparation and Evaluation of 1-Substituted 1,2,3,4-Tetrahydro- and 3,4-Dihydro-β-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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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.

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