Design, synthesis and biological evaluation of novel quinazoline derivatives as potential NF-κb inhibitors
| Autor: | Jing Pan, Long Ma, Yu-Xia Tang, Ying Tian, Yi-Hang Lin, Long-Jiang Zhang, Feng Gao, Guang-Ming Lu |
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| Jazyk: | angličtina |
| Rok vydání: | 2022 |
| Předmět: | |
| Zdroj: | Arabian Journal of Chemistry, Vol 15, Iss 7, Pp 103908- (2022) |
| Druh dokumentu: | article |
| ISSN: | 1878-5352 43936954 |
| DOI: | 10.1016/j.arabjc.2022.103908 |
| Popis: | 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. |
| Databáze: | Directory of Open Access Journals |
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