1125455-61-9Relevant articles and documents
Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment
Miller, Lori M.,Mayer, Scott C.,Berger, Dan M.,Boschelli, Diane H.,Boschelli, Frank,Di, Li,Du, Xuemei,Dutia, Minu,Floyd, Middleton B.,Johnson, Mark,Kenny, Cynthia Hess,Krishnamurthy, Girija,Moy, Franklin,Petusky, Susan,Tkach, Diane,Torres, Nancy,Wu, Biqi,Xu, Weixin
experimental part, p. 62 - 66 (2009/04/16)
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. Inhibitors of this receptor are believed to provide a new target in cancer therapy. We previously reported an isoquinolinedione series of IGF-1R inhibitors. Now we have identified a series of 3-cyanoquinoline compounds that are low nanomolar inhibitors of IGF-1R. The strategies, synthesis, and SAR behind the cyanoquinoline scaffold will be discussed.