Design, synthesis and biological evaluation of novel quinazoline derivatives as potential NF-κb inhibitors

Arabian Journal of Chemistry

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