1, 2, 3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors

R Tripathy, A Ghose, J Singh, ER Bacon…

Index: Tripathy, Rabindranath; Ghose, Arup; Singh, Jasbir; Bacon, Edward R.; Angeles, Thelma S.; Yang, Shi X.; Albom, Mark S.; Aimone, Lisa D.; Herman, Joseph L.; Mallamo, John P. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 6 p. 1793 - 1798

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Citation Number: 60

Abstract

KDR kinase inhibition is considered to play an important role in regulating angiogenesis, which is vital for the survival and proliferation of tumor cells. Recently we disclosed a structure-based kinase inhibitor design strategy which led to the identification of a new class of VEGFR-2/KDR kinase inhibitors bearing heterocyclic substituted pyrazolones as the core template. Instability in a rat S9 preparation and poor iv PK profiles for most of these ...