thienopyrimidine has been researched along with Edema* in 2 studies
2 other study(ies) available for thienopyrimidine and Edema
| Article | Year |
|---|---|
Design, synthesis and biological evaluation of some novel thienopyrimidines and fused thienopyrimidines as anti-inflammatory agents.
Some new substituted thienopyrimidine derivatives comprising thioxo, thioalkyl and pyrazolyl derivatives as well as fused thienotriazolopyrimidine and thienopyrimidinotriazine ring systems were prepared from 3-benzyl-2-hydrazino-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxamide 4. The designed compounds were evaluated for their anti-inflammatory activity. Compounds 4, 9, 10 and 13 showed the highest anti-inflammatory effect compared with the reference drug diclofenac sodium. Topics: Animals; Anti-Inflammatory Agents; Chemistry Techniques, Synthetic; Drug Design; Edema; Formaldehyde; Granuloma; Male; Pyrimidines; Rats; Triazoles; Turpentine; Ulcer | 2012 |
Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.
A series of novel thienopyrimidine-based receptor tyrosine kinase inhibitors has been discovered. Investigation of structure-activity relationships at the 5- and 6-positions of the thienopyrimidine nucleus led to a series of N,N'-diaryl ureas that potently inhibit all of the vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) receptor tyrosine kinases. A kinase insert domain-containing receptor (KDR) homology model suggests that these compounds bind to the "inactive conformation" of the enzyme with the urea portion extending into the back hydrophobic pocket adjacent to the adenosine 5'-triphosphate (ATP) binding site. A number of compounds have been identified as displaying excellent in vivo potency. In particular, compounds 28 and 76 possess favorable pharmacokinetic (PK) profiles and demonstrate potent antitumor efficacy against the HT1080 human fibrosarcoma xenograft tumor growth model (tumor growth inhibition (TGI) = 75% at 25 mg/kg.day, per os (po)). Topics: Adenosine Triphosphate; Animals; Antineoplastic Agents; Edema; Estradiol; Female; Humans; Mice; Mice, Inbred BALB C; Mice, SCID; Models, Molecular; NIH 3T3 Cells; Phosphorylation; Pyrimidines; Receptors, Platelet-Derived Growth Factor; Structure-Activity Relationship; Urea; Uterus; Vascular Endothelial Growth Factor Receptor-2; Xenograft Model Antitumor Assays | 2005 |