Synthesis of pyrrole-imidazole-duocarmycin polyamide and its sequence selective DNA alkylation. |
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| Authors: | T Fujiwara Z F Tao I Saito H Sugiyama |
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| Affiliation: | Institute for Medical and Dental Engineering, Tokyo Medical and Dental University, Japan. |
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| Abstract: | The new solid phase synthesis of sequence-specific DNA alkylating polyamides containing segment A of Du86 (Duo), N-methylimidazole (Im) and N-methylpyrrole (Py) amino acids is described. New monomer building block N-carboxylmethyl Py (Pyc) was synthesized from 2-methylpyrrolecarboxylate by eight steps. After normal coupling of FMOC-protected-Im and -Py monomer, the deprotection of silyl group generates free carboxylic acid. Introduction of various types of functional groups on solid support will be presented. |
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