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Solid-phase synthesis of novel inhibitors of Farnesyl Transferase

Lookup NU author(s): Dr Ian HardcastleORCiD

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Abstract

A novel diphosphate mimic, the 2,3,6-trifluoro-5-hydroxy-4-nitrophenoxy group (1), has been employed as the template in the solid-phase synthesis of novel Farnesyl Transferase inhibitors using the Mitsunobu reaction. The most potent inhibitor (farnesyloxy-5-hydroxy-2,3,6-trifluoro-4-nitrobenzene) displayed an IC₅₀ of 6.3 μM versus Farnesyl Transferase.

Publication metadata

Author(s): Barber AM, Hardcastle IR, Rowlands MG, Nutley BP, Marriott JH, Jarman M

Publication type: Article

Publication status: Published

Journal: Bioorganic & Medicinal Chemistry Letters

Year: 1999

Volume: 9

Issue: 4

Pages: 623-626

Print publication date: 09/04/1999

ISSN (print): 0960-894X

ISSN (electronic): 1464-3405

Publisher: Pergamon

URL: http://dx.doi.org/10.1016/S0960-894X(99)00043-8

DOI: 10.1016/S0960-894X(99)00043-8

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