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 ...
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[Fraley, Mark E; Rubino, Robert S; Hoffman, William F; Hambaugh, Scott R; Arrington, Kenneth L; Hungate, Randall W; Bilodeau, Mark T; Tebben, Andrew J; Rutledge, Ruth Z; Kendall, Richard L; McFall, Rosemary C; Huckle, William R; Coll, Kathleen E; Thomas, Kenneth A Bioorganic and medicinal chemistry letters, 2002 , vol. 12, # 24 p. 3537 - 3541]