Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology.
Bioorganic & Medicinal Chemistry Letters(2018)
摘要
•Discovery of potent, selective and orally bioavailable ERK inhibitor for oncology.•Synthesis of tert 3-(S)thiomethyl pyrrolidine based ERK inhibitors.•Improved PK due to sulfur substitution-mitigation of amide bond cleavage.
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关键词
ERK inhibitor,ATP competitive,MAP kinases,Kinase selectivity,Oncology
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