Discovery of Selective and Potent Macrocyclic CDK9 Inhibitors for the Treatment of Osimertinib-Resistant Non-Small-Cell Lung Cancer

Effectiveness of epidermal growth factor receptor (EGFR) inhibitors, including Osimertinib, for treating non-small-cell lung cancer (NSCLC) is limited due to the continuous emergence of drug resistance. Hence, it is urgent to develop new therapeutic approaches. CDK9, a key regulator of RNA transcrip...

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Veröffentlicht in:	Journal of medicinal chemistry 2023-11, Vol.66 (22), p.15340-15361
Hauptverfasser:	Wu, Tizhi, Yu, Bin, Xu, Yifan, Du, Zekun, Zhang, Zhiming, Wang, Yuxiao, Chen, Haoming, Zhang, Li Ao, Chen, Rui, Ma, Feihai, Gong, Weihong, Yu, Sixian, Qiu, Zhixia, Wu, Hongxi, Xu, Xi, Wang, Jubo, Li, Zhiyu, Bian, Jinlei
Format:	Artikel
Sprache:	eng
Schlagworte:	Aniline Compounds - pharmacology Aniline Compounds - therapeutic use Carcinoma, Non-Small-Cell Lung - drug therapy Cell Line, Tumor Cyclin-Dependent Kinase 9 Drug Resistance, Neoplasm ErbB Receptors - metabolism Humans Lung Neoplasms - drug therapy Macrocyclic Compounds - pharmacology Macrocyclic Compounds - therapeutic use Mutation Protein Kinase Inhibitors - pharmacology Protein Kinase Inhibitors - therapeutic use
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