Synthesis and biological evaluation of novel N-(alkoxyphenyl)-aminocarbonylbenzoic acid derivatives as PTP1B inhibitors

Yuan Feng Tong Pei Zhang Feng Chen Ling Hua Hao Fei Ye Jin Ying Tian Song Wu

引用本文: Yuan Feng Tong,  Pei Zhang,  Feng Chen,  Ling Hua Hao,  Fei Ye,  Jin Ying Tian,  Song Wu. Synthesis and biological evaluation of novel N-(alkoxyphenyl)-aminocarbonylbenzoic acid derivatives as PTP1B inhibitors[J]. Chinese Chemical Letters, 2010, 21(12): 1415-1418. doi: 10.1016/j.cclet.2010.07.005 shu
Citation:  Yuan Feng Tong,  Pei Zhang,  Feng Chen,  Ling Hua Hao,  Fei Ye,  Jin Ying Tian,  Song Wu. Synthesis and biological evaluation of novel N-(alkoxyphenyl)-aminocarbonylbenzoic acid derivatives as PTP1B inhibitors[J]. Chinese Chemical Letters, 2010, 21(12): 1415-1418. doi: 10.1016/j.cclet.2010.07.005 shu

Synthesis and biological evaluation of novel N-(alkoxyphenyl)-aminocarbonylbenzoic acid derivatives as PTP1B inhibitors

  • 基金项目:

    Financial support was provided by the National Natural Science Funds for Young Scholar (No.30901841),the Research Fund for the Doctoral Program of Higher Education of China (No.200800231145),and the Major Scientific and Technological Special Project for "Significant New Drugs Innovation" (No.2009ZX09301-003).

摘要: Based on the fact that petroselinic acid showed good inhibitory activity (IC50=6.99 μmol/L) against protein tyrosine phophatase 1B (PTP1B) in vitro, a series of novel N-(alkoxyphenyl)-aminocarbonylbenzoic acid derivatives were designed and synthesized. The results indicated that most of the derivatives showed more potent activities against PTP1B. Especially, compound 13 had obvious activity with an IC50 of 106 nmol/L in vitro.

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  • 收稿日期:  2010-04-08
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