Optimization of a pyrazolo [1, 5-a] pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics

ME Fraley, RS Rubino, WF Hoffman…

Index: Bioorganic and medicinal chemistry letters, , vol. 12, # 24 p. 3537 - 3541

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Citation Number: 78

Abstract

... Bioorganic & Medicinal Chemistry Letters. ... Departments of Medicinal Chemistry and Cancer ... The chemistry in the 3-phenyl series involved oxidation of the corresponding 4-pyridyl ring followed by rearrangement of the resulting pyridine n-oxide under standard conditions ...