Novel tricyclic aminoacetyl and sulfonamide inhibitors of Ras farnesyl protein transferase

Novel tricyclic FPT inhibitors with submicromolar FPT activity are described. Greatly enhanced FPT activity is realized with phthaloyl derivatized amino compound 2k, which showed FPT inhibitory activity of IC 50 = 0.66 μM. Sulfonamides 5g and 50 were also found to be potent FPT inhibitor. SAR result...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1996-12, Vol.6 (24), p.2977-2982
Main Authors: Njoroge, F.George, Vibulbhan, Bancha, Alvarez, Carmen S., Bishop, W.Robert, Petrin, Joanne, Doll, Ronald J., Girijavallabhan, V., Ganguly, Ashit K.
Format: Article
Language:English
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Summary:Novel tricyclic FPT inhibitors with submicromolar FPT activity are described. Greatly enhanced FPT activity is realized with phthaloyl derivatized amino compound 2k, which showed FPT inhibitory activity of IC 50 = 0.66 μM. Sulfonamides 5g and 50 were also found to be potent FPT inhibitor. SAR resulting from a variety of tricyclic amino acids and sulfonamide derivatives is discussed. Novel 8-chlorobenzocycloheptapyridine aminoacetyl and sulfonamide inhibitors of ras farnesyl protein transferase are described. These compounds are nonsulfhydryl and nonpeptidic in nature.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(96)00558-6