Bioorganic & Medicinal Chemistry Letters 2005-12-01

Nonsteroidal anti-inflammatory drugs and their analogues as inhibitors of aldo-keto reductase AKR1C3: new lead compounds for the development of anticancer agents.

Stanislav Gobec, Petra Brozic, Tea Lanisnik Rizner

文献索引：Bioorg. Med. Chem. Lett. 15 , 5170-5, (2005)

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摘要

Nonsteroidal anti-inflammatory drugs (NSAIDs) like indomethacin, flufenamic acid, and related compounds have been recently identified as potent inhibitors of AKR1C3. We report that some other NSAIDs (diclofenac and naproxen) also inhibit AKR1C3, with the IC(50) values in the low micromolar range. In order to obtain more information about the structure-activity relationship and to identify new leads, a series of compounds designed on the basis of NSAIDs were synthesized and screened on AKR1C3. The most active compounds were 2-[(2,2-diphenylacetyl)amino]benzoic acid 4 (IC(50)=11microM) and 3-phenoxybenzoic acid 10 (IC(50)=0.68microM). These compounds represent promising starting points for the development of new anticancer agents.

相关化合物

  • 萘普生
  • 对乙酰氨基苯酚
  • 3-苯氧基苯甲酸
  • 阿司匹林
  • 邻苯甲酰苯甲酸
  • 4-甲基二苯甲酮
  • 双氯芬酸钠
  • 酮洛芬
  • 非那西丁
  • 布洛芬

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