Abstract
Eleven novel 4-anilinoquinazoline derivatives were synthesized and evaluated for their invitro antiproliferative activity. Among them, compound 9a exhibited the best potency, with IC50 values of 25-682nm against various types of cancer cell lines. In addition, 9a was confirmed that it could arrest the cell cycle at G2 /M phase and trigger apoptosis. Indirect immunofluorescence staining revealed its antitubulin property. Importantly, 9a significantly inhibited tumor growths in SM-7721 xenograft models (57.0% tumor mass change) without causing significant loss of body weight, suggesting that 9a is a promising new anticancer agent to be developed.
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