Studies on Aromatase Inhibitors. III. Synthesis and Biological Evaluation of [(4-Bromobenzyl)(4-cyanophenyl)amino]azoles and Their Azine Analogs

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概要

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• A series of [(4-bromobenzyl)(4-cyanophenyl)amino]azoles and their azine analogs, which have the side chain of the selective aromatase inhibitor YM511,were synthesized and evaluated for aromatase-inhibitory activity (in vivo) and for pregnant mare serum gonadotropin (PMSG)-induced estrogen synthesis inhibitory activity (in vitro). Among these aza-heterocycles, the pyrimidin-5-yl derivative (6a) was the most potent aromatase inhibitor and its in vitro inhibitory activity was comparable to that of YM511. Compound 6a also showed weak inhibitory activity on aldosterone synthesis. These data indicated that the pyrimidin-5-yl moiety is useful as a new azole fragment in place of the 4H-1,2,4-triazol-4-yl moiety of the aromatase inhibitor YM511.

• 公益社団法人日本薬学会の論文
• 1997-03-15

著者

• Okada M

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• KUDOH Masafumi

  Metabolic Diseases Research, Pharmacology Laboratories, Institute for Drug Discovery Research, Yaman

• Isomura Y

  Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn

• OKADA Minoru

  Medical Chemistry Research II, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co.,

• YODEN Toru

  Medical Chemistry Research II, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co.,

• KAWAMINAMI Eiji

  Medical Chemistry Research II, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co.,

• ISOMURA Yasuo

  Medical Chemistry Research II, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co.,

• SHIMADA Yoshiaki

  Medicinal Chemistry Research III, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical C

• SHIMADA Yasuo

  Mitsuboshi Pharmacutical Co.

• Yoden T

  Institute For Technology Development Yamanouchi Pharmaceutical Co. Ltd.

• Shimada Y

  Mitsuboshi Pharmaceutical Co

• Kudoh Masafumi

  Drug Discovery Research Astellas Pharma Inc.

• Kawaminami Eiji

  Medicinal Chemistry Research Ii Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co.

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