Tricyclic Farnesyl Protein Transferase Inhibitors: Crystallographic and Calorimetric Studies of Structure−Activity Relationships †
✍ Scribed by Strickland, Corey L.; Weber, Patricia C.; Windsor, William T.; Wu, Zhen; Le, Hung V.; Albanese, Margaret M.; Alvarez, Carmen S.; Cesarz, David; del Rosario, Joycelyn; Deskus, Jeffrey; Mallams, Alan K.; Njoroge, F. George; Piwinski, John J.; Remiszewski, Stacy; Rossman, Randall R.; Taveras, Arthur G.; Vibulbhan, Bancha; Doll, Ronald J.; Girijavallabhan, Viyyoor M.; Ganguly, Ashit K.
- Book ID
- 124058993
- Publisher
- American Chemical Society
- Year
- 1999
- Tongue
- English
- Weight
- 255 KB
- Volume
- 42
- Category
- Article
- ISSN
- 0022-2623
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Novel Tricyclic Aminoacetyl and Sulfonamide Inhibitors of RAS Farnesyl Protein Transferase. -It is shown that derivatization of the amino group with a phthaloyl moiety increases inhibitory activity of the title compounds, cf. (IIIc) and (IIId). The potent inhibitors (III) and (V) are non-peptidic,