5-(4-methoxybenzylidene)thiazolidine-2-4-dione has been researched along with Neoplasms* in 2 studies
2 other study(ies) available for 5-(4-methoxybenzylidene)thiazolidine-2-4-dione and Neoplasms
| Article | Year |
|---|---|
5-(4-Methoxybenzylidene)thiazolidine-2,4-dione-derived VEGFR-2 inhibitors: Design, synthesis, molecular docking, and anticancer evaluations.
A novel series of 5-(4-methoxybenzylidene)thiazolidine-2,4-dione derivatives, 5a-g and 7a-f, was designed, synthesized, and evaluated for their anticancer activity against HepG2, HCT116, and MCF-7 cells. HepG2 and HCT116 were the most sensitive cell lines to the influence of the new derivatives. In particular, compounds 7f, 7e, 7d, and 7c were found to be the most potent derivatives of all the tested compounds against the HepG2, HCT116, and MCF-7 cancer cell lines. Compound 7f (IC Topics: Antineoplastic Agents; Doxorubicin; HCT116 Cells; Hep G2 Cells; Humans; Inhibitory Concentration 50; MCF-7 Cells; Molecular Docking Simulation; Neoplasms; Protein Kinase Inhibitors; Sorafenib; Structure-Activity Relationship; Thiazolidinediones; Vascular Endothelial Growth Factor Receptor-2 | 2020 |
Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases.
The Pim protein kinases are frequently overexpressed in prostate cancer and certain forms of leukemia and lymphoma. 5-(3-Trifluoromethylbenzylidene)thiazolidine-2,4-dione (4a) was identified by screening to be a Pim-1 inhibitor and was found to attenuate the autophosphorylation of tagged Pim-1 in intact cells. Although 4a is a competitive inhibitor with respect to ATP, a screen of approximately 50 diverse protein kinases demonstrated that it has high selectivity for Pim kinases. Computational docking of 4a to Pim-1 provided a model for lead optimization, and a series of substituted thiazolidine-2,4-dione congeners was synthesized. The most potent new compounds exhibited IC(50)s of 13 nM for Pim-1 and 2.3 microM for Pim-2. Additional compounds in the series demonstrated selectivities of more than 2500-fold and 400-fold for Pim-1 or Pim-2, respectively, while other congeners were essentially equally potent toward the two isozymes. Overall, these compounds are new Pim kinase inhibitors that may provide leads to novel anticancer agents. Topics: Animals; Antineoplastic Agents; Cell Line; Cell-Free System; Combinatorial Chemistry Techniques; Female; Humans; Kinetics; Mice; Mice, Inbred BALB C; Models, Molecular; Molecular Structure; Neoplasm Transplantation; Neoplasms; Phosphorylation; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-pim-1; Structure-Activity Relationship; Thiazolidinediones | 2009 |