Bioorganic and Medicinal Chemistry Letters p. 703 - 708 (1999)
Update date:2022-08-03
Topics:
Shen, Wang
Fakhoury, Stephen
Donner, Greg
Henry, Kenneth
Lee, Jang
Zhang, Haichao
Cohen, Jerry
Warner, Robert
Saeed, Badr
Cherian, Sajeev
Tahir, Stephen
Kovar, Peter
Bauch, Joy
Ng, Shi-Chung
Marsh, Kennan
Sham, Hing
Rosenberg, Saul
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.
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