CBI ANALOGUES OF CC-1065 AND THE DUOCARMYCINS

摘要

132 CBI analogues of CC-1 065 and the duocarmycins having dimeric monocyclic, bicyclic, and tricyclic heteroaromatics substituents were synthesized by a parallel route. The resultant analogues were evaluated with respect to their catalytic and cytotoxic activities. The relative contribution of the various dimeric monocyclic, bicyclic, and tricyclic heteroaromatics substituents within the DNA binding domain were characterized. Several of the resultant CBI analogues of CC-1065 and the duocarmycins were characterized as having enhanced catalytic and cytotoxic activities and were identified as having utility as anti-cancer agents.