Analyze how specific documents activate the features of the SAE. Select a dataset, a run and a document to begin.
1551
Details List
Document Content
2,4-Diaminopyrimidine inhibitors of c-Met kinase bearing benzoxazepine anilines.
Elaboration of the SAR around a series of 2,4-diaminopyrimidines led to a number of c-Met inhibitors in which kinase selectivity was modulated by substituents appended on the C4-aminobenzamide ring and the nature of the C2-aminoaryl ring. Further lead optimization of the C2-aminoaryl group led to benzoxazepine analogs whose pharmaceutical properties were modulated by the nature of the substituent on the benzoxazepine nitrogen. Tumor stasis (with partial regressions) were observed when an orally bioavailable analog was evaluated in a GTL-16 tumor xenograft mouse model. Subsequent PK/PD studies suggested that a metabolite contributed to the overall in vivo response.
Similar Documents
-
#34 0.673Methylglyoxal bis(butylamidinohydrazone) exhibits…
-
#805 0.670Characterization of the human cytochrome P450 for…
-
#535 0.663Synthesis and cytotoxicity evaluation of biaryl-b…
-
#370 0.663Discovery of potent and selective phenylalanine d…
-
#519 0.657Multi-substituted 8-aminoimidazo[1,2-a]pyrazines …