Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2018-03-19 , DOI: 10.1016/j.bmc.2018.03.029 Takahiro Inoue , Osamu Shimozato , Nina Matsuo , Yusuke Mori , Yoshinao Shinozaki , Jason Lin , Takayoshi Watanabe , Atsushi Takatori , Nobuko Koshikawa , Toshinori Ozaki , Hiroki Nagase
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:
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。。