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

Mark E. Fraley, Robert S. Rubino, William F. Hoffman, Scott R. Hambaugh, Kenneth L. Arrington, Randall W. Hungate, Mark T. Bilodeau, Andrew J. Tebben, Ruth Z. Rutledge, Richard Kendall,

Bioorganic & Medicinal Chemistry Letters · 2002 · 87 citations · 13 references

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13

Inhibition of vascular endothelial growth factor-induced angiogenesis suppresses tumour growth in vivo

K. Jin Kim, Bing Li, Jane Winer et al. · Nature · 1993 · 3.6K citations

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Dormancy of micrometastases: Balanced proliferation and apoptosis in the presence of angiogenesis suppression

Lars Holmgren, Michael S. O’Reilly, Judah Folkman · Nature Medicine · 1995 · 1.9K citations

, , +14

SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularization, and growth of multiple tumor types.

T. Annie T. Fong, Laura K. Shawver, Li Sun et al. · PubMed · 1999 · 1K citations

, , +16

Regulation of angiogenesis via vascular endothelial growth factor receptors.

Tanja Veikkola, Marika J. Karkkainen, Lena Claesson‐Welsh et al. · PubMed · 2000 · 745 citations

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Synthesis and Secretion of Vascular Permeability Factor/Vascular Endothelial Growth Factor by Human Retinal Pigment Epithelial Cells

A.P. Adamis, David T. Shima, K T Yeo et al. · Biochemical and Biophysical Research Communications · 1993 · 400 citations

, , +10