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Bioorg Chem ; 148: 107450, 2024 Jul.
Article in English | MEDLINE | ID: mdl-38761704

ABSTRACT

Here, a series of 3-(6-aminopyridin-3-yl) benzamide derivatives were designed and synthesized. Cell viability assay indicated that most compounds exhibited potent antiproliferative activity against all the tested cancer cells. Among them, compound 7l displayed the best antiproliferative activity particularly in A549 cells, with an IC50 value of 0.04 ± 0.01 µM. RNA-seq analysis was employed to explore the potential pathways related to the antiproliferative activity of compound 7l. The data revealed that 7l exerted antiproliferative activity mainly by regulating cell cycle, DNA replication and p53 signaling pathway. Indeed, compound 7l induced G2/M phase arrest by AURKB transcription inhibition and resulted in cell apoptosis via p53 signaling pathway. Most importantly, compound 7l demonstrated potent antitumor activity in A549 xenograft tumor model. Collectively, 7l might be a promising lead compound for the development of new therapeutic agents for AURKB overexpressed or mutated cancers.


Subject(s)
Antineoplastic Agents , Apoptosis , Benzamides , Cell Cycle Checkpoints , Cell Proliferation , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Humans , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Apoptosis/drug effects , Benzamides/pharmacology , Benzamides/chemical synthesis , Benzamides/chemistry , Cell Proliferation/drug effects , Structure-Activity Relationship , Molecular Structure , Cell Cycle Checkpoints/drug effects , Animals , Mice , Mice, Nude , Cell Line, Tumor , Protein Kinase Inhibitors/pharmacology , Protein Kinase Inhibitors/chemical synthesis , Protein Kinase Inhibitors/chemistry , Transcription, Genetic/drug effects , Mice, Inbred BALB C
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