Article
Discovery of Selective and Potent Macrocyclic CDK9 Inhibitors for the Treatment of Osimertinib-Resistant Non-Small-Cell Lung Cancer.
Journal of medicinal chemistry - 23 Nov 2023
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
Abstract excerpt
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 transcription, has emerged as a promising target for the development of antitumor drugs due to its crucial role in modulating...
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