Lead identification to generate isoquinolinedione inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment

…, G Krishnamurthy, K Kutterer, F Moy, S Petusky…

文献索引：Mayer, Scott C.; Banker, Annette L.; Boschelli, Frank; Di, Li; Johnson, Mark; Kenny, Cynthia Hess; Krishnamurthy, Girija; Kutterer, Kristina; Moy, Franklin; Petusky, Susan; Ravi, Malini; Tkach, Diane; Tsou, Hwei-Ru; Xu, Weixin Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 12 p. 3641 - 3645

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被引用次数: 42

摘要

Insulin-like growth factor receptor (IGF-1R) is a growth factor receptor tyrosine kinase that acts as a critical mediator of cell proliferation and survival. This receptor is over-expressed or activated in tumor cells and is emerging as a novel target in cancer therapy. Efforts in our “Hit to Lead” group have generated a novel series of submicromolar IGF-1R inhibitors based on a isoquinolinedione template originating from a Lance enzyme HTS screen. Chemical ...