Design, synthesis and pharmacological evaluation of 2-arylurea-1,3,5-triazine derivative (XIN-9): A novel potent dual PI3K/mTOR inhibitor for cancer therapy

A class of 2-arylurea-1,3,5-triazine derivatives (A1-A28) were designed and synthesized. The derivative A9 (XIN-9) with excellent inhibitory activity was screened to be a promising PI3K/mTOR dual inhibitor. [Display omitted] •A novel series 2-arylurea-1, 3, 5-triazine derivatives were designed and c...

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Veröffentlicht in:	Bioorganic chemistry 2022-12, Vol.129, p.106157-106157, Article 106157
Hauptverfasser:	Sun, Xin, Zhang, Binliang, Luo, Leixuan, Yang, Yang, He, Bin, Zhang, Qian, Wang, Linxiao, Xu, Shan, Zheng, Pengwu, Zhu, Wufu
Format:	Artikel
Sprache:	eng
Schlagworte:	2-arylurea-1,3,5-triazine Antineoplastic Agents - chemistry Cell Line, Tumor Cell Proliferation Cytotoxicity Humans Inhibitor Molecular Docking Simulation MTOR Inhibitors Neoplasms - drug therapy Phosphatidylinositol 3-Kinases - metabolism Phosphoinositide-3 Kinase Inhibitors - pharmacology PI3K/mTOR Protein Kinase Inhibitors - pharmacology Proto-Oncogene Proteins c-akt - metabolism Signal Transduction Structure-activity relationship TOR Serine-Threonine Kinases - metabolism Triazines - pharmacology
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