To examine the hydrophobic structure of PI polyamides on tumor accumulation in vivo, PI polyamide-fluorescein conjugates 1–5 with the distinct number of N-methylimidazole (Im) units were synthesized. There existed an inverse relationship between the Im unit number of the compounds and their hydrophobicity. Compound 1 with one Im unit and 3 with three Im units accumulated and retained preferentially in tumor tissues compared to 5 with five Im units. These results suggest the importance of a PI polyamide’s primary structure, which partly contributes to its hydrophobic property, on its accumulation and/or retention in tumor tissues in vivo.

中文翻译：

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发夹十环吡咯-咪唑聚酰胺的疏水结构增强体内肿瘤组织的积累/保留

为了检查PI聚酰胺对肿瘤积累的疏水性结构体内，PI聚酰胺-荧光素缀合物1 - 5与的不同数目Ñ甲基咪唑（IM）单位被合成。化合物的Im单位数与它们的疏水性之间存在反比关系。与具有五个Im单元的5个化合物相比，具有1个Im单元的化合物1和具有三个Im单元的化合物3优先积累并保留在肿瘤组织中。这些结果表明PI聚酰胺的一级结构的重要性，该一级结构对其疏水性，体内在肿瘤组织中的积累和/或滞留有部分贡献。。