Solid-phase synthesis of novel inhibitors of farnesyl transferase

A M Barber; I R Hardcastle; M G Rowlands; B P Nutley; J H Marriott; M Jarman

doi:10.1016/s0960-894x(99)00043-8

Solid-phase synthesis of novel inhibitors of farnesyl transferase

Bioorg Med Chem Lett. 1999 Feb 22;9(4):623-6. doi: 10.1016/s0960-894x(99)00043-8.

Authors

A M Barber¹, I R Hardcastle, M G Rowlands, B P Nutley, J H Marriott, M Jarman

Affiliation

¹ Cancer Research Campaign Laboratory, CRC Centre for Cancer Therapeutics at the Institute of Cancer Research, Sutton, Surrey, UK.

PMID: 10098677
DOI: 10.1016/s0960-894x(99)00043-8

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 microM versus farnesyl transferase.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Alkyl and Aryl Transferases / antagonists & inhibitors*
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology
Farnesyltranstransferase

Substances

Enzyme Inhibitors
Alkyl and Aryl Transferases
Farnesyltranstransferase