化学
生物利用度
药理学
乳腺癌
激酶
三阴性乳腺癌
细胞生长
癌症研究
癌症
内科学
生物化学
医学
作者
Wenjing Wang,Lixin Gao,Simei Wang,Wensi Huang,Xinyu Meng,Hao Hu,Ziqiang Chen,Jingya Sun,Guangpeng Liu,Yubo Zhou,Xingxing Diao,Ruimin Huang,Jia Li,Xiaohua Chen
标识
DOI:10.1021/acs.jmedchem.4c00233
摘要
Triple-negative breast cancer (TNBC) represents a highly aggressive and heterogeneous malignancy. Currently, effective therapies for TNBC are very limited and remain a significant unmet clinical need. Targeting the transcription-regulating cyclin-dependent kinase 9 (CDK9) has emerged as a promising avenue for therapeutic treatment of TNBC. Herein, we report the design, synthesis, optimization, and evaluation of a new series of aminopyrazolotriazine compounds as orally bioavailable, potent, and CDK9/2 selectivity-improved inhibitors, enabling efficacious inhibition of TNBC cell growth, as well as notable antitumor effect in TNBC models. The compound
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