e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521
8-Substituted O6-benzylguanine, substituted 6 (4)-(benzyloxy) pyrimidine, and related derivatives as inactivators of human O6-alkylguanine-DNA alkyltransferase
The ability of these compounds to inactivate the AGT protein in HT29 human colon tumor cell extracts and in intact HT29 cells is summarized in Table 1. The data represent the dose of compound required to produce 50% inactivation in cell-free extracts upon incubation for 30 min or in cells upon incubation for 4 h. These ED50 values were obtained from plots of the percent alkyltransferase activity remaining as a function of dose of compound ...
