Diaryl ether inhibitors of farnesyl-protein transferase.

Bioorg Med Chem Lett

Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486. USA.

Published: May 2001

AI Article Synopsis

  • Imidazolemethyl diaryl ethers effectively inhibit farnesyl-protein transferase (FPTase), making them significant in biochemical research.
  • A SNAr displacement reaction technique allowed for the fast, parallel synthesis of various FPTase inhibitors.
  • Testing a wide array of commercially available phenols helped identify active compounds in cellular environments.

Article Abstract

Imidazolemethyl diaryl ethers are potent inhibitors of farnesyl-protein transferase. The SNAr displacement reaction used to prepare these diaryl ethers was amenable to rapid parallel synthesis of FPTase inhibitors. The use of a broad range of commercially available phenols quickly identified compounds which proved active in cells.

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Source
http://dx.doi.org/10.1016/s0960-894x(01)00162-7DOI Listing

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