Abstract
A series of methylthiazonaphthalimides was synthesized and quantitatively evaluated as efficient DNA intercalators, antitumor agents and DNA photocleavers. A 1 showed both efficient antitumor activities against cell lines of A549 and P388 with IC 50 of 82.8 and 31 nM, respectively. A 3 was the strongest antitumor agent against A549 with the IC 50 of 20.8 nM. A 2 , the most efficient DNA intercalator, was found to be the strongest DNA photocleaver via superoxide anion. An explanation was given for the disaccord between antitumor and DNA photocleaving activities.
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