Potent Inhibitors Of Protein Farnesyltransferase: Heteroarenes As Cysteine Replacements

W Shen,S Fakhoury,G Donner,K Henry,J Lee,Hc Zhang,J Cohen,R Warner,B Saeed,S Cherian,S Tahir,P Kovar,J Bauch,S C Ng,K Marsh,H Sham,S Rosenberg

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（1999）

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摘要

Synthesis and biological evaluation of heteroarenes as reduced cysteine replacements are described. Of the heteroaryl groups examined with respect to FT inhibitor FTI-276 (1), pyridyl was the replacement found to be most effective. Substitutions at C4 of the pyridyl moiety did not affect the in vitro activity. Compound 9a was found to have moderate in vivo bioavailability. (C) 1999 Elsevier Science Ltd. All rights reserved.

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关键词

protein farnesyltransferase,potent inhibitors,heteroarenes

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