Arabian Journal of Chemistry | |
Design, synthesis and biological evaluation of novel quinazoline derivatives as potential NF-κb inhibitors | |
Feng Gao1  Jing Pan2  Yi-Hang Lin2  Yu-Xia Tang2  Long Ma2  Ying Tian2  Long-Jiang Zhang2  Guang-Ming Lu3  | |
[1] Corresponding authors.;Department of Medical Imaging, Jinling Hospital, School of Medicine, Nanjing University, Nanjing, China;Haina Precision Machining Research Center, Yangtze Delta Region Research Institute of Tsinghua University, Zhejiang, China; | |
关键词: 4-aminoquinazoline; Molecular docking; Anticancer activity; NF-κb; Breast cancer; | |
DOI : | |
来源: DOAJ |
【 摘 要 】
A series of novel 4-aminoquinazoline derivatives were designed, synthesized and biological properties on nuclear factor-kappaB (NF-κb) pathway inhibitory and potential in vitro anti-proliferation against breast cancer lines were also evaluated. Among them, LU1501 exhibited potent inhibition with IC50 values in SK-BR-3 (10.16 ± 0.86 µM) and HCC1806 (10.66 ± 1.01 µM) cell lines. In vivo studies in breast cancer tumor model proved the correlation between anticancer activity of LU1501 and proliferation inhibition through the NF-κb signal pathway. The molecular docking studies also portrayed the potential binding mechanism between LU1501 and the key proteins of p65 and IkBα in NF-κb pathway. Accordingly, compound LU1501 could serve as a potent agent against breast cancer for further investigation.
【 授权许可】
Unknown