Synthesis and Biological Evaluation of Novel Substituted 4‐Anilinoquinazolines as Antitumor Agents | Zendy

Cao Dong | Zendy; Wang Xiaoyan | Zendy; Lei Lei | Zendy; Ma Liang | Zendy; Yang Zhuang | Zendy; Wang Fang | Zendy; Chen Lijuan | Zendy

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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.

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