化学
赫拉
细胞毒性
噻唑
细胞毒性T细胞
MTT法
噻吩
立体化学
细胞培养
吉非替尼
A549电池
体外
生物化学
表皮生长因子受体
有机化学
受体
生物
遗传学
作者
Kamala K. Vasu,Chander Singh Digwal,Amit N. Pandya,Dhaivat H. Pandya,Jayesh A. Sharma,Sneha Patel,Milee Agarwal
标识
DOI:10.1016/j.bmcl.2017.10.060
摘要
A series of new imidazo[1,2-a]pyridine linked with thiazole/thiophene motif through a keto spacer were synthesized and tested for their cytotoxic potential against three human cancer cell lines including A549, HeLa and U87-MG using MTT assay. Compounds A2, A3, A4, C1 and C2 showed cytotoxicity against all the three cell lines. The selectivity index for compound A4 for A549 and HeLa cells was comparable to that of doxorubicin. Among the synthesized compounds, B5 showed the maximum inhibition of NF-κB activity as ascertained by NF-κB reporter assay (IC50 = 6.5 ± 0.6 µM). Treatment of NCI-H23 cells (EGFR overexpressed, KRAS G12V mutant) with erlotinib and gefitinib along with compounds A4 and B5 indicated synergistic and additive potential of combination therapy.
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