N-Alkylated 1,4-Dihydropyridines : New Agents to Overcome Multidrug Resistance

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概要

• 論文の詳細を見る

• New N-alkylated 1,4-dihydropyridine derivatives were synthesized and their ability to overcome multidrug resistance was examined in vincristine-resistant P388 cells (P388/VCR cells). Compounds that possessed an arylalkyl substituent on the dihydropyridine ring nitrogen were more potent than verapamil in potentiating the cytotoxicity of vincristine against P388/VCR cells. However, neither drug effectively enhanced the antitumor activity of vincristine in tumor-bearing mice. Introduction of basic nitrogen-containing substituents on the side chain of 1,4-dihydropyridines gave improved activity in vitro and in vivo. The piperazine derivative 12c and 12o were more than 10 times as potent as verapamil in vitro. Four compounds selected for in vivo testing showed superior antitumor activity in P388/VCR-bearing mice in combination with vincristine. The structure-activity relationships of the compounds are discussed.

• 社団法人日本薬学会の論文
• 1995-05-15

著者

• 辻 尚志

  Central Research Laboratories Ajinomoto Co. Inc.

• 鶴尾 隆

  Institute Of Molecular And Cellular Biosciences University Of Tokyo

• Akiyama Yohko

  Faculty Of Pharmaceutical Sciences Chiba University

• 大角 幸治

  Central Research Laboratories, Ajinomoto Co., Inc.,

• 大石 和夫

  Central Research Laboratories, Ajinomoto Co., Inc.,

• 森永 芳弘

  Central Research Laboratories, Ajinomoto Co., Inc.,

• 中川 隆佑

  Central Research Laboratories, Ajinomoto Co., Inc.,

• 須賀 泰世

  Central Research Laboratories, Ajinomoto Co., Inc.,

• 関山 隆顕

  Central Research Laboratories, Ajinomoto Co., Inc.,

• 秋山 由紀夫

  Central Research Laboratories, Ajinomoto Co., Inc.,

• 大石 和夫

  Central Research Laboratories Ajinomoto Co. Inc.

• Ogura K

  Kobe Pharmaceutical University

• 須賀 泰世

  Central Research Laboratories Ajinomoto Co. Inc.

• Suga Y

  Central Research Laboratories Ajinomoto Co. Inc.

• 大角 幸治

  Central Research Laboratories Ajinomoto Co. Inc.

• Ohsumi Koji

  Central Research Laboratories Ajinomoto Co. Inc.

• 秋山 由紀夫

  Roussel Morishita Co. Ltd. Shiga Jpn

• 中川 隆佑

  Central Research Laboratories Ajinomoto Co. Inc.

• 森永 芳弘

  Central Research Laboratories Ajinomoto Co. Inc.

• 関山 隆顕

  Central Research Laboratories Ajinomoto Co. Inc.

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