Synthesis and Initial SAR Studies of 3,6-Disubstituted Pyrazolo[1,5-a]pyrimidines: A New Class of KDR Kinase Inhibitors

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• 作者：Fraley ; Mark E. ; Hoffman ; William F. ; Rubino ; Robert S. ; Hungate ; Randall W. ; Tebben ; Andrew J. ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2002
• 出版时间：October 7, 2002
• 年：2002
• 卷：12
• 期：1
• 页码：2767-2770
• 全文大小：141 K

文摘

We have synthesized and evaluated the activity of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines as a new class of KDR kinase inhibitors. Starting with screening lead 1, potency against isolated KDR was fully optimized with 3-thienyl and 4-methoxyphenyl substituents at the 6- and 3-positions (3g, KDR IC₅₀