Synthesis and Biological Evaluation of Quinocarcin Derivatives

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概要

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• Cyanation of quinocarcin readily opened the oxazolidine ring to provide DX-52-1 (2), which was a key compound in the synthesis of quinocarcin derivatives. Various electrophilic reactions toward aromatic ring of DX-52-1 were examined, and 10-substituted (e.g., halogen, nitro, formyl, cyano, hydroxy, etc.) analogs were prepared. Dehydrocyanation of the derivatives could be achieved to reproduce the oxazolidine ring upon treatment with HCl or AgNO_3. 10-Chloride 10 and 10-bromide 11 were the most promising among the derivatives prepared. Antitumor activity of 10 was extended to B-16 melanoma.

• 社団法人日本薬学会の論文
• 1990-05-25

著者

• 森本 眞

  Pharmaceutical Research Laboratories

• 平田 正

  Tokyo Research Laboratories Kyowa Hakko Kogyo Co. Ltd.

• 佐藤 章

  Kyowa Hakko Kogyo Co. Ltd. Tokyo Research Laboratories

• 宇於崎 洋一

  Kyowa Hakko Kogyo Co. Ltd. Tokyo Research Laboratories

• 斉藤 博満

  Kyowa Hakko Kogyo Co., Ltd., Tokyo Research Laboratories

• 芦沢 忠

  Pharmaceutical Research Laboratories

• 平田 正

  Kyowa Hakko Kogyo Co., Ltd., Tokyo Research Laboratories

• 小林 茂

  Kyowa Hakko Kogyo Co., Ltd., Tokyo Research Laboratories

• 藤本 和久

  Pharmaceutical Research Laboratories

• 三好 勝則

  Pharmaceutical Research Laboratories

• 斉藤 博満

  Kyowa Hakko Kogyo Co. Ltd. Tokyo Research Laboratories

• 小林 茂

  Kyowa Hakko Kogyo Co. Ltd. Tokyo Research Laboratories

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