新規遺伝子発現制御化合物としてのピロールポリアミド-ヌクレオシドハイブリッド及びそのハイブリッドを組込んだオリゴマーの設計，合成及び評価

摘要: On the basis of reports that a minor groove binder pyrrolepolyamide can interfere with gene expression by sequence-specific recognition DNA, we expected nucleoside bearing would be able to regulate expression. Therefore, designed and synthesized pyrrolepolyamide-adenosine (Hybrid 1) -2′-deoxyguanosine hybrids 2 Hybrid 3) as lead compounds for control compounds. The frame 3 combines at 2-exocyclic amino group 2′-deoxyguanosine linker guanine exists in side duplex. is 2′-deoxyguanosine-pyrrolepolyamide hybrid using 3-aminopropionyl linker, while uses 3-aminopropyl linker. An evaluation DNA binding sequence selectivity was performed analysis Tm values CD spectra, distamycin A contrast. has provided more excellent sequence-distinguishable ability than other Distamycin A. Moreover, on these results, oligonucleotides conjugated 4, which stable under conditions oligonucleotide solid phase synthesis, arranged from 3. From spectral analysis, it found conjugating 4 possess high very includes sequence.