473416-22-7Relevant articles and documents
HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS
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Paragraph 0449, (2021/01/23)
Heterocyclic compounds as CDK4 or CDK6 or other CDK inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology
Boga, Sobhana Babu,Alhassan, Abdul-Basit,Cooper, Alan B.,Doll, Ronald,Shih, Neng-Yang,Shipps, Gerald,Deng, Yongqi,Zhu, Hugh,Nan, Yang,Sun, Robert,Zhu, Liang,Desai, Jagdish,Patel, Mehul,Muppalla, Kiran,Gao, Xiaolei,Wang, James,Yao, Xin,Kelly, Joseph,Gudipati, Subrahmanyam,Paliwal, Sunil,Tsui, Hon-Chung,Wang, Tong,Sherborne, Bradley,Xiao, Li,Hruza, Alan,Buevich, Alexei,Zhang, Li-Kang,Hesk, David,Samatar, Ahmed A.,Carr, Donna,Long, Brian,Black, Stuart,Dayananth, Priya,Windsor, William,Kirschmeier, Paul,Bishop, Robert
, p. 2029 - 2034 (2018/05/16)
Compound 5 (SCH772984) was identified as a potent inhibitor of ERK1/2 with excellent selectivity against a panel of kinases (0/231 kinases tested @ 100 nM) and good cell proliferation activity, but suffered from poor PK (rat AUC PK @10 mpk = 0 μM h; F% =