169250-92-4Relevant academic research and scientific papers
Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
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, (2008/06/13)
A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: STR1 to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds of formulas 5.0, 5.1 and 5.2, wherein R is --C(R20)(R21)(R46), and 5.3, 5.3A and 5.3B, wherein R is --N(R25)(R48), are disclosed. Also disclosed are processes for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3. Further disclosed are novel compounds which are intermediates in the process for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3.
Discovery of novel nonpeptide tricyclic inhibitors of ras farnesyl protein transferase
Njoroge, F. George,Doll, Ronald J.,Vibulbhan, Bancha,Alvarez, Carmen S.,Bishop, W. Robert,Petrin, Joanne,Kirschmeier, Paul,Carruthers, Nicholas I.,Wong, Jesse K.,Albanese, Margaret M.,Piwinski, John J.,Catino, Joseph,Girijavallabhan,Ganguly, Ashit K.
, p. 101 - 113 (2007/10/03)
A comprehensive structure-activity relationship (SAR) study of novel tricyclic amides has been undertaken. The discovery of compounds that are potent FPT inhibitors in the nanomolar range has been achieved. These compounds are nonpeptidic and do not contain sulfhydryl groups. They selectively inhibit farnesyl protein transferase (FPT) and not geranylgeranyl protein transferase-1 (GGPT-1). They also inhibit H-Ras processing in Cos monkey kidney cells.
Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
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, (2008/06/13)
Novel compounds of Formula (7.0a), (7.0b) or (7.0c): STR1 are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the formula (7.0a), (7.0b) or (7.0c) to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.
