2. Academic Validation
  3. Synthesis and antitumor activity of novel 6,7,8-trimethoxy N-aryl-substituted-4-aminoquinazoline derivatives

Synthesis and antitumor activity of novel 6,7,8-trimethoxy N-aryl-substituted-4-aminoquinazoline derivatives

  • Bioorg Med Chem Lett. 2018 Aug 1;28(14):2561-2565. doi: 10.1016/j.bmcl.2018.05.033.
Fang Liu 1,  Ziyou Huai 2,  Guotai Xia 1,  Liuping Song 2,  Sha Li 1,  Yulan Xu 1,  Kangjun Hong 1,  Mingyue Yao 2,  Gang Liu 3,  Yinjiu Huang 4
Affiliations

Affiliations

  • 1 School of Pharmacy, Bengbu Medical College, Anhui Engineering Technology Research Center of Biochemical Pharmaceuticals, Bengbu 233030, Anhui, PR China.
  • 2 Department of Bioscience, Bengbu Medical College, Bengbu 233030, Anhui, PR China.
  • 3 School of Chemistry and Materials Science, Ludong University, Yantai 264000, Shandong, PR China. Electronic address: shdliugang@163.com.
  • 4 Department of Bioscience, Bengbu Medical College, Bengbu 233030, Anhui, PR China. Electronic address: yinjiuhuang1973@163.com.
PMID: 29903662 DOI: 10.1016/j.bmcl.2018.05.033
Abstract

A series of 6,7,8-trimethoxy N-aryl-substituted-4-aminoquinazoline derivatives were synthesized as epidermal growth factor receptor (EGFR) inhibitors, and their antitumor activities were assessed in the gastric Cancer cell line SGC7901 using MTT assay. All compounds of Tg1-14 were found to inhibit SGC7901 cell proliferation, and compound Tg11 (IC50 = 0.434 μM) was found to be slightly more effective against SGC7901 cells than epirubicin (IC50 = 5.16 μM). This suggests that compound Tg11 can be used as a new substitution structure to develop more efficacious antitumor agents. Western blot analysis showed that treatment with Tg11 (40 μM for 30 min) resulted in near complete inhibition of EGF-induced ERK1/2 phosphorylation, indicating that its anti-proliferative effect is largely associated with inhibition of ERK1/2 activation. These data imply that Tg11 is a potential Anticancer agent capable of inhibiting cell proliferation.

Keywords

4-Anilinoquinazoline; Antitumor; Epidermal growth factor receptor (EGFR); Synthesis.

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