The discovery of kinase inhibitors by a combination of diversity-oriented synthesis and selective screening

We herein report the synthesis, biological activity and preliminary structure-activity relationships of a series of diaryl[1,3]diazepines. These compounds were able to inhibit the proliferation of many cancer cell lines, such as HeLa, MCF-7, SGC7901 and A549. When HeLa cells were treated with lead compounds 7j and 7k at 3 [Formula: see text] concentration, cell arrest was observed in the G2/M phase.

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Synthesis and structure–activity relationship study of diaryl[d,f][1,3]diazepines as potential anti-cancer agents

Yan

Wang

Chen

et al. 2018

Mol Divers

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Design, synthesis, and pharmacological evaluation of quinazoline derivatives as novel and potent pan-JAK inhibitors

Xiang

Wang

et al. 2023

Bioorganic Chemistry

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The discovery of kinase inhibitors by a combination of diversity-oriented synthesis and selective screening

Abstract: An efficient strategy for the discovery of kinase inhibitors by a combination of diversity-oriented synthesis and selective screening was presented.

Cited by 2 publications

References 42 publications

Synthesis and structure–activity relationship study of diaryl[d,f][1,3]diazepines as potential anti-cancer agents

Synthesis and structure–activity relationship study of diaryl[d,f][1,3]diazepines as potential anti-cancer agents

Design, synthesis, and pharmacological evaluation of quinazoline derivatives as novel and potent pan-JAK inhibitors

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