二茂铁的嘌呤和嘌呤等排衍生物：ADME、抗肿瘤和电化学性质的评估。
Purine and Purine Isostere Derivatives of Ferrocene: An Evaluation of ADME, Antitumor and Electrochemical Properties.
机构信息
Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Zagreb 10000, Croatia.
Fidelta d.o.o., Zagreb 10000, Croatia.
出版信息
Molecules. 2020 Mar 29;25(7):1570. doi: 10.3390/molecules25071570.
Novel purine and purine isosteres containing a ferrocene motif and 4,1-disubstituted (-, -, -, -, -, , -, -, -) and 1,4-disubstituted (- and -) 1,2,3-triazole rings were synthesized. The most potent cytotoxic effect on colorectal adenocarcinoma (SW620) was exerted by the 6-chloro-7-deazapurine (IC = 9.07 µM), 6-chloropurine (IC = 14.38 µM) and (IC = 15.50 µM) ferrocenylalkyl derivatives. The -9 isomer of 6-chloropurine containing ferrocenylmethylene unit showed a favourable in vitro physicochemical and ADME properties including high solubility, moderate permeability and good metabolic stability in human liver microsomes.
合成了含有二茂铁基和 4,1-二取代（-, -, -, -, -,, -, -, -) 和 1,4-二取代（- 和 -) 1,2,3-三唑环的新型嘌呤和嘌呤类似物。6-氯-7-脱氮嘌呤（IC = 9.07 µM）、6-氯嘌呤（IC = 14.38 µM）和（IC = 15.50 µM）二茂铁烷基衍生物对结直肠腺癌（SW620）表现出最强的细胞毒性作用。含有二茂铁亚甲基单元的 6-氯嘌呤的-9 异构体具有有利的体外理化和 ADME 特性，包括高溶解度、适度的通透性和良好的人肝微粒体代谢稳定性。
Zotero 插件