Synthesis of new 4-anilinoquinazoline analogues and evaluation of their EGFR inhibitor activity.

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.

[Study on the chemical changes of whole constituents in the preparing process of kansui root].

OBJECTIVE: To study the chemical changes of whole constituents in the preparing process of kansui root in order to uncover the mechanism of detoxication in preparing process. METHODS: The raw and prepared kansui were extracted with water and methanol and analyzed with HPLC respectively. RESULTS: Seven constituents disappeared in the prepared kansui and four new consitituents were produced in the water extracts. The concentration of four other constituents decreased. In the methoanol extract, two constituents disappeared and one constituent produced during preparing process. The concentration of six other constituents increased in the methanol extracts. CONCLUSION: The mechanism of detoxication of kansui root preparing process is may be that the toxic constituents decomposing or water solubility reducing.