Synthesis of aryl-heteroaryl ureas (AHUs) based on 4-aminoquinoline and their evaluation against the insulin-like growth factor receptor (IGF-1R)

W Engen, TE O'Brien, B Kelly, J Do, L Rillera…

Index: Engen, William; O'Brien, Terrence E.; Kelly, Brendan; Do, Jacinda; Rillera, Liezel; Stapleton, Lance K.; Youngren, Jack F.; Anderson, Marc O. Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 16 p. 5995 - 6005

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Citation Number: 13

Abstract

The insulin-like growth factor receptor (IGF-1R) is a receptor tyrosine kinase (RTK) involved in all stages of the development and propagation of breast and other cancers. The inhibition of IGF-1R by small molecules remains a promising strategy to treat cancer. Herein, we explore SAR around previously characterized lead compound (1), which is an aryl- heteroaryl urea (AHU) consisting of 4-aminoquinaldine and a substituted aromatic ring ...