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- W308386567 abstract "Based on the structural feature of nonclassical antifolates, a series of 4 (3H)-quinazolinone derivatives bearing aromatic amine side chains have been designed by incorporating trimethoxyphenyl, an antitumor pharmacophore, with 4 (3H)-quinazolinone. N-alkylation of 3,4,5-trimethoxyphenylamine with appropriate amount of alkyl halides afforded 4 kinds of N-substituted 3,4,5-trimethoxyphenylamines in 30.3%~60.6% yields. The target compounds 8a 8m were obtained through the reactions of 6-bromo-2-methyl-4 (3H)-quinazolinone with 3,4,5-trimethoxyphenylamine, N-substituted 3,4,5-trimethoxyphenylamines or other arylamines at room temperature in 30.8%~71.9% yields, and their structures were confirmed by means of ESIMS, 1H NMR, elemental analysis or HRMS. The in vitro cytotoxicities against A-549 (human non-small cell lung cancer), HCT-8 (human colon cancer) and Bel-7402 (human liver cancer) cell lines of the synthesized compounds 8a~8m were tested with colorimetric MTT assay, and the results indicated that the percent growth inhibition against A-549, HCT-8 and Bel-7402 cell lines at 5×10^(-6)g/mL concentration of the compounds 8a~8m were all lower than 25%." @default.
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- W308386567 date "2007-02-10" @default.
- W308386567 modified "2023-09-23" @default.
- W308386567 title "4(3H)-喹唑啉酮芳胺衍生物的合成及其抗肿瘤活性评价" @default.
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