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- W2057491145 abstract "Novel diphosphonate homologs7a–7c,and their cyclic counterparts8a–8c,of the previously synthesized farnesyl pyrophosphate analogs1and2were prepared and tested for their inhibition potency and specificity of the enzymes PFT and PGGT-I. Compound2was shown to be the most potent inhibitor of PFT (IC50= 0.58 ± 0.45 μM) in this series. The novel compound7a,the one carbon homolog of2,proved to be the most potent inhibitor of PGGT-I (IC50= 0.98 ± 0.01 μM). The cyclic analogs8a–8care generally less biologically active. The compounds2and7aare nonspecific toward inhibition of PFT and PGGT-I and may inhibit both farnesylation and geranylgeranylation processing of oncogenic proteins." @default.
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- W2057491145 date "1998-11-01" @default.
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- W2057491145 title "Inhibitors of Protein:Farnesyl Transferase and Protein:Geranylgeranyl Transferase I: Synthesis of Homologous Diphosphonate Analogs of Isoprenylated Pyrophosphate" @default.
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- W2057491145 doi "https://doi.org/10.1006/bioo.1998.1101" @default.
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