Tailor-made Antitumor Agents based on DNA Sequence

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Direct regulation of the expression level of a specific gene will provide a promising approach for cancer therapy. N-Methylpyrrole (Py) and N-methylimidazole (Im) polyamides are a new type of small molecules that precisely bind to the minor groove of the DNA duplex in a sequence-specific fashion. We designed and synthesized a series of sequence-specific alkylating Py-Im polyamide conjugates that selectively alkylate taget DNA sequences. We have demonstrated that sequence-specific alkylating agents possess gene-silencing activities and a promising potency against human cancer cell lines.