Optimization of a pyrazolo [1, 5-a] pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics
…, WF Hoffman, SR Hambaugh, KL Arrington…
文献索引：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
We have introduced solubilizing functionality to a 3, 6-disubstituted pyrazolo [1, 5-a] pyrimidine series of KDR kinase inhibitors to improve the physical properties of these compounds. The addition of a basic side-chain to the 6-aryl ring, introduction of 3-pyridyl groups, and most significantly, incorporation of a 4-pyridinonyl substituent at the 6-position of the core are modifications that maintain and often enhance the intrinsic potency of this ...
