Imidazo[1,2-a]pyridines linked with thiazoles/thiophene motif through keto spacer as potential cytotoxic agents and NF-κB inhibitors.
作者： Kamala K. Vasu , Chander Singh Digwal , Amit N. Pandya , Dhaivat H. Pandya , Jayesh A. Sharma
DOI: 10.1016/J.BMCL.2017.10.060
关键词:
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 U87-MG using MTT assay. Compounds A2, A3, A4, C1 C2 showed cytotoxicity all the lines. The selectivity index compound A4 A549 cells was comparable to that doxorubicin. Among compounds, B5 maximum inhibition NF-κB activity as ascertained by reporter assay (IC50 = 6.5 ± 0.6 µM). Treatment NCI-H23 (EGFR overexpressed, KRAS G12V mutant) erlotinib gefitinib along compounds indicated synergistic additive combination therapy.
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