Synthesis of new 4-anilinoquinazoline analogues and evaluation of their EGFR inhibitor activity / 药学学报

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.

Comparative study of MSCT and pathological findings of solitary pulmonary nodules / 重庆医学

Objective To evaluate the diagnostic value of MSCT in Solitary Pulmonary Nodules (SPN) with different pathologic types .Methods Four-five SPN with pathological findings including 16 benign cases and 29 malignant cases were retrospectively an-alyzed ,and performed with MSCT scanning .Observation of the distribution ,morphology and internal characteristics of SPN by post-processing technique were done ,and the results were compared with pathological findings .Results Among 45 SPN ,the benign nodules included 6 cases of inflammatory pseudotumor ,4 cases of tuberculoma ,3 cases of hamartoma ,2 cases of cryptococcus and 1 case of hemangioendothelioma ,and the malignant nodules included 21 cases of adenocarcinoma ,3 cases of squamous carcinoma ,2 ca-ses of small cell carcinoma and 3 cases of alveolar cell carcinoma .Average diameter of benign nodules was 2 .1 cm ,and 2 .6 cm for the malignant nodules .All SPN ,including 5 cases in the inner zone ,12 in the medial zone and 28 in the lateral zone ,the percentages with malignant signs at the corresponding parts were 40% (2/5) ,50% (6/12) ,75% (21/28) ,there was significant difference be-tween distributions(P0 .05);the incidences of leaf sign ,burr sign ,pleural indentation sign ,cavitas and bronchial air sign ,blood vessels cluster sign of malignant nodules were higher than that of the benign nodules(P<0 .05) ,and the inflammatory pseudotumor and adenocarcinoma owned similar characteristics ;the incidence of calcification in tuberculoma and hamartoma was high ,while cavitas in tuberculosis and lung cancer were high .Conclusion MSCT can sufficiently display the distribution ,morphology and internal characteristics of SPN , and can help make qualitative diagnosis of benign and malignant SPN ,providing great practical value in clinical treatment .