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Synthesis and Biological Evaluation of Novel Substituted 4‐Anilinoquinazolines as Antitumor Agents
Author(s) -
Cao Dong,
Wang Xiaoyan,
Lei Lei,
Ma Liang,
Yang Zhuang,
Wang Fang,
Chen Lijuan
Publication year - 2020
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12706
Subject(s) - apoptosis , in vitro , potency , chemistry , cell cycle , cell cycle checkpoint , cell culture , cytotoxicity , tubulin , staining , immunofluorescence , cancer research , microbiology and biotechnology , biochemistry , biology , microtubule , antibody , immunology , genetics
Eleven novel 4‐anilinoquinazoline derivatives were synthesized and evaluated for their in vitro antiproliferative activity. Among them, compound 9a exhibited the best potency, with IC 50 values of 25−682 n m against various types of cancer cell lines. In addition, 9a was confirmed that it could arrest the cell cycle at G 2 /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.