Synthesis and preliminary biological evaluation of the derivatives of O6-benzylguanine as inactivators of O6-alkylguanine-DNA alkyltransferase

A series of new O6-BG derivatives (14–21,23–30) were synthesized as inactivators of O6-Alkylguanine-DNA alkyltransferase (AGT), and their ability to inhibit AGT was preliminary evaluated by MTT with O6-BG as the control. The result suggested compound 30 displayed a higher activity than O6-BG.