Discovery of 3 H-benzo [4, 5] thieno [3, 2-d] pyrimidin-4-ones as potent, highly selective, and orally bioavailable inhibitors of the human protooncogene proviral …

ZF Tao, LA Hasvold, JD Leverson, EK Han…

文献索引：Tao, Zhi-Fu; Hasvold, Lisa A.; Leverson, Joel D.; Han, Edward K.; Guan, Ran; Johnson, Eric F.; Stoll, Vincent S.; Stewart, Kent D.; Stamper, Geoff; Soni, Nirupama; Bouska, Jennifer J.; Luo, Yan; Sowin, Thomas J.; Lin, Nan-Horng; Giranda, Vincent S.; Rosenberg, Saul H.; Penning, Thomas D. Journal of Medicinal Chemistry, 2009 , vol. 52, # 21 p. 6621 - 6636

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被引用次数: 67

摘要

Pim-1, Pim-2, and Pim-3 are a family of serine/threonine kinases which have been found to be overexpressed in a variety of hematopoietic malignancies and solid tumors. Benzothienopyrimidinones were discovered as a novel class of Pim inhibitors that potently inhibit all three Pim kinases with subnanomolar to low single-digit nanomolar Ki values and exhibit excellent selectivity against a panel of diverse kinases. Protein crystal structures of ...