su-11248 and Leukemia--Myeloid

su-11248 has been researched along with Leukemia--Myeloid* in 1 studies

Other Studies

1 other study(ies) available for su-11248 and Leukemia--Myeloid

Article	Year
Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. Bioorganic & medicinal chemistry, 2010, Jul-01, Volume: 18, Issue:13 A series of new ureidoindolin-2-one derivatives were synthesized and evaluated as inhibitors of receptor tyrosine kinases. Investigation of structure-activity relationships at positions 5, 6, and 7 of the oxindole skeleton led to the identification of 6-ureido-substituted 3-pyrrolemethylidene-2-oxindole derivatives that potently inhibited both the vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) families of receptor tyrosine kinases. Several derivatives showed potency against the PDGFR inhibiting both its enzymatic and cellular functions in the single-digit nanomolar range. Among them, compound 35 was a potent inhibitor against tyrosine kinases, including VEGFR and PDGFR families, as well as Aurora kinases. Inhibitor 36 (non-substituted on the pyrrole or phenyl ring) had a moderate pharmacokinetic profile and completely inhibited tumor growth initiated with the myeloid leukemia cell line, MV4-11, in a subcutaneous xenograft model in BALB/c nude mice. Topics: Animals; Aurora Kinases; Binding Sites; Cell Line, Tumor; Computer Simulation; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Indoles; Leukemia, Myeloid; Mice; Oxindoles; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Pyrroles; Receptors, Platelet-Derived Growth Factor; Structure-Activity Relationship; Transplantation, Heterologous; Urea	2010

Article

Year

Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors.

Bioorganic & medicinal chemistry, 2010, Jul-01, Volume: 18, Issue:13

A series of new ureidoindolin-2-one derivatives were synthesized and evaluated as inhibitors of receptor tyrosine kinases. Investigation of structure-activity relationships at positions 5, 6, and 7 of the oxindole skeleton led to the identification of 6-ureido-substituted 3-pyrrolemethylidene-2-oxindole derivatives that potently inhibited both the vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) families of receptor tyrosine kinases. Several derivatives showed potency against the PDGFR inhibiting both its enzymatic and cellular functions in the single-digit nanomolar range. Among them, compound 35 was a potent inhibitor against tyrosine kinases, including VEGFR and PDGFR families, as well as Aurora kinases. Inhibitor 36 (non-substituted on the pyrrole or phenyl ring) had a moderate pharmacokinetic profile and completely inhibited tumor growth initiated with the myeloid leukemia cell line, MV4-11, in a subcutaneous xenograft model in BALB/c nude mice.

Topics: Animals; Aurora Kinases; Binding Sites; Cell Line, Tumor; Computer Simulation; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Indoles; Leukemia, Myeloid; Mice; Oxindoles; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Pyrroles; Receptors, Platelet-Derived Growth Factor; Structure-Activity Relationship; Transplantation, Heterologous; Urea

2010