Design, Synthesis, Formulation, and Bioevaluation of Trisubstituted Triazines as Highly Selective mTOR Inhibitors for the Treatment of Human Breast Cancer

The aberrant activation of the PI3K/mTOR signaling pathway is implicated in various human cancers. Thus, the development of inhibitors targeting mTOR has attracted considerable attention. In this study, we used a structure-based drug design strategy to discover a highly potent and kinase-selective m...

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Veröffentlicht in:	Journal of medicinal chemistry 2024-05, Vol.67 (9), p.7330-7358
Hauptverfasser:	Sun, Qiwen, Chu, Yuxiu, Zhang, Nana, Chen, Rui, Wang, Lili, Wu, Jiangxia, Dong, Yongxi, Li, Hongliang, Wang, Ling, Tang, Lei, Zhan, Changyou, Zhang, Ji-Quan
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use Autophagy - drug effects Breast Neoplasms - drug therapy Breast Neoplasms - pathology Cell Proliferation - drug effects Drug Design Female Humans MCF-7 Cells Mice Mice, Inbred BALB C Mice, Nude MTOR Inhibitors - chemical synthesis MTOR Inhibitors - chemistry MTOR Inhibitors - pharmacology MTOR Inhibitors - therapeutic use Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacokinetics Protein Kinase Inhibitors - pharmacology Protein Kinase Inhibitors - therapeutic use Structure-Activity Relationship TOR Serine-Threonine Kinases - antagonists & inhibitors TOR Serine-Threonine Kinases - metabolism Triazines - chemical synthesis Triazines - chemistry Triazines - pharmacokinetics Triazines - pharmacology Triazines - therapeutic use Xenograft Model Antitumor Assays
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