Promoted by the fact that the topoisomerases are promising targets of anticancer drugs, and of those expressing a topoisomerase-targeting activity, the synthetic analogues of alkaloid family of Benzo[c]phenanthroline (BCP) are weel studied, this work focused on development of a way to obtain the BCP analogues with 1 or 2 nitrogen atoms in the cycle A, with or without ethoxyl groups in position 12. The following three compounds 8,9-dimethoxybenzo[c][1,9]phenanthrolin (12), 12-ethoxy-8,9-dimethoxy benzo[c][1,9] phenanthrolin (13), 8,9-dimethoxypyridazino[4,5c]phenanthridin (14) were synthesized by cyclization via intermediates of benzyne. In-vitro cytoxicity tests on L 1210 cell line showed these compounds were more potent than fagaronin, a natural BCP containing an aromatic cycle A in structure.
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