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Thirteen of 4-anilinoquinazoline derivatives with imine groups at position 6 of quinazoline ring were synthesized and their antitumor activities were evaluated by MTT assay and Western blotting analysis. Among these compounds, 13a-131 were reported first time. The MTT assay was carried out on three human cancer cell lines (A549, HepG2 and SMMC7721) with EGFR highly expressed. Among the tested compounds, 13i and 13j exhibited notable inhibition potency and their IC50 values on three cell lines were equivalent to or less than those of gefitinib. Compound 14, without imine group substituted, displayed excellent inhibitor potency only on A549 cell line. Compounds 14 and 13j were chosen to perform Western blotting analysis on A549. The results showed that both of the compounds could inhibit the expression level of phosphorylated EGFR remarkably. It was concluded that the inhibitor potency of compound 14 was almost equivalent to that of gefitinib and the inhibitor potency of 13j was better than that of gefitinib.
Zheng Wang, and
Cui-Ling WANG, and
Jun-lin Li, and
Ning Zhang, and
Yan-ni Sun, and
Zhu-lan Liu, and
Zhi-shu Tang, and
Jian-li Liu
November 2007,
Bioorganic & medicinal chemistry letters,
Zheng Wang, and
Cui-Ling WANG, and
Jun-lin Li, and
Ning Zhang, and
Yan-ni Sun, and
Zhu-lan Liu, and
Zhi-shu Tang, and
Jian-li Liu
September 2007,
Bioorganic & medicinal chemistry,
Zheng Wang, and
Cui-Ling WANG, and
Jun-lin Li, and
Ning Zhang, and
Yan-ni Sun, and
Zhu-lan Liu, and
Zhi-shu Tang, and
Jian-li Liu
November 2009,
Organic & biomolecular chemistry,
Zheng Wang, and
Cui-Ling WANG, and
Jun-lin Li, and
Ning Zhang, and
Yan-ni Sun, and
Zhu-lan Liu, and
Zhi-shu Tang, and
Jian-li Liu
January 2016,
Anti-cancer agents in medicinal chemistry,
Zheng Wang, and
Cui-Ling WANG, and
Jun-lin Li, and
Ning Zhang, and
Yan-ni Sun, and
Zhu-lan Liu, and
Zhi-shu Tang, and
Jian-li Liu
November 2019,
European journal of medicinal chemistry,
Zheng Wang, and
Cui-Ling WANG, and
Jun-lin Li, and
Ning Zhang, and
Yan-ni Sun, and
Zhu-lan Liu, and
Zhi-shu Tang, and
Jian-li Liu
January 2005,
Journal of chemical information and modeling,
Zheng Wang, and
Cui-Ling WANG, and
Jun-lin Li, and
Ning Zhang, and
Yan-ni Sun, and
Zhu-lan Liu, and
Zhi-shu Tang, and
Jian-li Liu
April 2017,
European journal of medicinal chemistry,
Zheng Wang, and
Cui-Ling WANG, and
Jun-lin Li, and
Ning Zhang, and
Yan-ni Sun, and
Zhu-lan Liu, and
Zhi-shu Tang, and
Jian-li Liu
October 2017,
Research in pharmaceutical sciences,
Zheng Wang, and
Cui-Ling WANG, and
Jun-lin Li, and
Ning Zhang, and
Yan-ni Sun, and
Zhu-lan Liu, and
Zhi-shu Tang, and
Jian-li Liu
June 2009,
Bioorganic & medicinal chemistry letters,
Zheng Wang, and
Cui-Ling WANG, and
Jun-lin Li, and
Ning Zhang, and
Yan-ni Sun, and
Zhu-lan Liu, and
Zhi-shu Tang, and
Jian-li Liu
January 2015,
Bioorganicheskaia khimiia,
