Solid-phase synthesis of novel inhibitors of farnesyl transferase |
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| Authors: | Barber A M Hardcastle I R Rowlands M G Nutley B P Marriott J H Jarman M |
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| Affiliation: | Cancer Research Campaign Laboratory, CRC Centre for Cancer Therapeutics at the Institute of Cancer Research, Sutton, Surrey, UK. |
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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 microM versus farnesyl transferase. |
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