Structure-Activity Relationships of Diamines, Dicarboxamides, and Disulfonamides on Vinblastine Accumulation in P388/ADR Cells

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概要

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• Diamines, dicarboxamides, and disulfonamides that have terminal benzene, methyl- or chloro-substituted benzene rings were synthesized and evaluated for the activity of [^3H]vinblastine accumulation in multidrug-resistant P388/ADR cells. The efficacy of these compounds was generally in the order of dicarboxamides<diamines<disulfonamides. N-Methylated diamine and disulfonamide compounds having terminal methyl- or chloro-substituted benzene rings in their structure also showed rather potent efficacy. From these findings, we synthesized a novel disulfonamide compound, 1,2,3,4,5,6-hexahydro-2,5-bis(p-toluenesulfonyl)benzo[2,5]diazocine (22). Compound 22 suppressed the efflux of vinblastine from P388/ADR cells and increased its intracellular accumulation, while it barely increased the vinblastine accumulation in sensitive cells (P388/S). Compound 22 significantly potentiated the growth-inhibitory effects of vinblastine, vincristine, colchicine and Adriamycin against P388/ADR cells in vitro.

• 社団法人日本薬学会の論文
• 1994-07-15

著者

• 宮本 謙一

  金沢大学 大学院医学系研究科 循環医科学専攻

• 宮本 謙一

  金沢大学薬学部

• 田中 憲一

  Faculty Of Pharmaceutical Sciences Hokuriku University

• 涌澤 伸哉

  Faculty of Pharmaceutical Sciences, Hokuriku University

• 宮本 謙一

  Faculty of Pharmaceutical Sciences, Hokuriku University

• 澤西 啓之

  Faculty of Pharmaceutical Sciences, Hokuriku University

• 村上 理枝子

  Faculty of Pharmaceutical Sciences, Hokuriku University

• 吉藤 茂行

  Faculty of Pharmaceutical Sciences, Hokuriku University

• 吉藤 茂行

  Faculty Of Pharmaceutical Sciences Of Hokuriku University

• 涌沢 伸哉

  北陸大 薬

• 涌澤 伸哉

  Faculty Of Pharmaceutical Sciences Hokuriku University

• 村上 理枝子

  Faculty Of Pharmaceutical Sciences Hokuriku University

• Yoshifuji Shigeyuki

  Faculty Of Pharmaceutical Sciences Of Hokuriku University

• 吉藤 茂行

  Faculty Of Pharmaceutical Sciences Hokuriku University

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