当前位置: X-MOL 学术Pharm. Chem. J. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Cytotoxic Activity of Perfluoroalkyl-Substituted Imidazoindazoles and Imidazobenzisoxazoles
Pharmaceutical Chemistry Journal ( IF 0.8 ) Pub Date : 2021-06-14 , DOI: 10.1007/s11094-021-02401-4
T. S. Khlebnikova , O. V. Panibrat , Yu. A. Piven , V. G. Zinovich , E. M. Tumar , S. E. Ogurtsova , F. A. Lakhvich

The cytotoxic activity of perfluoroalkyl imidazoindazoles and imidazobenzisoxazoles with respect to MCF-7 (human breast carcinoma) and HepG2 cell lines (human hepatocellular carcinoma) was studied. The imidazoindazoles exhibited significant cytotoxicity against MCF-7 and HepG2 cell lines. 2,6-bis(4-Fluorophenyl)-4,4-dimethyl-8-trifluoromethyl-3,4,5,6-tetrahydroimidazo[4,5-e]indazole displayed the most pronounced cytotoxic action. Regioisomeric imidazobenzisoxazoles inhibited extensively growth of HepG2 cells. The mechanism of cytotoxic action can be related to the induction of apoptosis as a result of disruption of the cell cycle, in particular, arrest of HepG2 cells in the G2 phase and MCF-7 cells in the G1 phase.



中文翻译:

全氟烷基取代的咪唑并吲唑和咪唑并苯并异恶唑的细胞毒活性

研究了全氟烷基咪唑并吲唑和咪唑苯并异恶唑对 MCF-7(人乳腺癌)和 HepG2 细胞系(人肝细胞癌)的细胞毒活性。咪唑并吲唑对 MCF-7 和 HepG2 细胞系表现出显着的细胞毒性。2,6-(4-氟苯基)-4,4-二甲基-8-三氟甲基-3,4,5,6-四氢咪唑并[4,5- e ]吲唑表现出最显着的细胞毒作用。区域异构的咪唑并苯并异恶唑可广泛抑制 HepG2 细胞的生长。细胞毒作用的机制可能与细胞周期中断导致的细胞凋亡诱导有关,特别是 HepG2 细胞在 G2 期和 MCF-7 细胞在 G1 期的停滞。

更新日期:2021-06-14
down
wechat
bug