二氢茚并异喹啉作为茚并异喹啉的前药发挥作用。
Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.
作者信息
Xiao Xiangshu, Miao Ze-Hong, Antony Smitha, Pommier Yves, Cushman Mark
机构信息
Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, IN 47907, USA.
出版信息
Bioorg Med Chem Lett. 2005 Jun 2;15(11):2795-8. doi: 10.1016/j.bmcl.2005.03.101.
Dihydroindenoisoquinolines are analogs of cytotoxic indenoisoquinoline topoisomerase I (Top1) inhibitors, exhibiting potent cytotoxicity but weak inhibitory activity toward Top1. Through COMPARE analysis, cytotoxicity studies in Top1-deficient cells, chemical synthesis and biological evaluation of methylated dihydroindenoisoquinoline 5, we demonstrated that dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines in cancer cells.
二氢茚并异喹啉是细胞毒性茚并异喹啉拓扑异构酶I（Top1）抑制剂的类似物，具有强大的细胞毒性，但对Top1的抑制活性较弱。通过比较分析、对Top1缺陷细胞的细胞毒性研究、甲基化二氢茚并异喹啉5的化学合成及生物学评估，我们证明二氢茚并异喹啉在癌细胞中作为茚并异喹啉的前药发挥作用。
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