Synthesis of Novel Curcumin Analogues and Their Evaluation as Selective Cyclooxygenase-1 (COX-1) Inhibitors

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概要

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• Curcumin, a major yellow pigment and active component of turmeric, has been shown to possess anti-inflammatory and anti-cancer activities. Recent studies have indicated that cyclooxygenase-1 (COX-1) plays an important role in inflammation and carcinogenesis. In order to find more selective COX-1 inhibitors a series of novel curcumin derivatives was synthesized and evaluated for their ability to inhibit this enzyme using in vitro inhibition assays for COX-1 and COX-2 by measuring PGE_2 production. All curcumin analogues showed a higher rate of COX-1 inhibition. The most potent curcumin compounds were (1E,6E)-1,7-di-(2,3,4-trimethoxyphenyl)-1,6-heptadien-3,5-dione (4) (COX-1: IC50=0.06μM, COX-2: IC_<50>>100μM, selectivity index>1666) and (1E,6E)-methyl 4-[7-(4-methoxycarbonyl)phenyl]-3,5-dioxo-1,6-heptadienyl]benzoate (6) (COX-1: IC_<50>=0.05μM, COX-2: IC_<50>>100μM, selectivity index>2000). Curcumin analogues therefore represent a novel class of highly selective COX-1 inhibitors and promising candidates for in vivo studies.

• 2007-01-01

著者

• Erker Thomas

  Department Of Medicinal Chemistry University Of Vienna

• HANDLER Norbert

  Department of Medicinal Chemistry, University of Vienna

• JAEGER Walter

  Department of Clinical Pharmacy and Diagnostics, University of Vienna

• PUSCHACHER Helmut

  Department of Medicinal Chemistry, University of Vienna

• LEISSER Klaus

  Department of Medicinal Chemistry, University of Vienna

• Leisser Klaus

  Department Of Medicinal Chemistry University Of Vienna

• Jaeger Walter

  Department Of Clinical Pharmacy And Diagnostics University Of Vienna

• Handler Norbert

  Department Of Medicinal Chemistry University Of Vienna

• Puschacher Helmut

  Department Of Medicinal Chemistry University Of Vienna

関連論文

• Effects of Novel Synthesized Pyridothiazines on Various Guinea Pig Heart Muscle Preparations(Pharmacology)
• Synthesis of Novel Curcumin Analogues and Their Evaluation as Selective Cyclooxygenase-1 (COX-1) Inhibitors

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