Synthesis of N2-(substituted benzyl)-3-(4-methylphenyl)indazoles as novel anti-angiogenic agents

Li Jiau Huang, Mei Ling Shih, Hua Sin Chen, Shiow Lin Pan, Che Ming Teng, Fang Yu Lee, Sheng Chu Kuo

研究成果: 雜誌貢獻文章同行評審

82 引文 斯高帕斯(Scopus)

摘要

To search for novel compounds with potent anti-angiogenic activity, a series of N1-(substituted benzyl)-3-(4-methylphenyl)-1H-indazoles (16, 18, 20, 22, 24, 26, 28, 30, 32) and N2-(substituted benzyl)-3-(4-methylphenyl)-2H-indazoles (17, 19, 21, 23, 25, 27, 29, 31, and 33) were synthesized. The structures of these regioisomers were established by IR, UV, and NMR spectral data. 3-(4-Methylphenyl)-1H-indazole (6) and the N 2-substituted derivatives (17, 19, 21, 23, 25, 29, 31, 33) were evaluated for their anti-angiogenic activity. Most of them showed more prominent activity than ethyl 4-(1-benzyl-1H-indazol-3-yl)benzoate (YD-3). Among these tested compounds, 2-(4-chlorobenzyl)-3-(4-methylphenyl)-2H-indazole (19), 2-(4-methylbenzyl)-3-(4-methylphenyl)-2H-indazole (25), and 2-(4-methoxybenzyl)- 3-(4-methylphenyl)-2H-indazole (31) showed significant anti-angiogenic activity and are worthy of further investigation.
原文英語
頁(從 - 到)528-536
頁數9
期刊Bioorganic and Medicinal Chemistry
14
發行號2
DOIs
出版狀態已發佈 - 1月 15 2006

ASJC Scopus subject areas

  • 藥物發現
  • 分子醫學
  • 分子生物學
  • 生物化學
  • 臨床生物化學
  • 藥學科學
  • 有機化學

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