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Synthesis of pyrrole-imidazole-duocarmycin polyamide and its sequence selective DNA alkylation.
Authors:T Fujiwara  Z F Tao  I Saito  H Sugiyama
Affiliation:Institute for Medical and Dental Engineering, Tokyo Medical and Dental University, Japan.
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.
Keywords:
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