5-(4-methoxybenzylidene)thiazolidine-2-4-dione has been researched along with 2-4-thiazolidinedione* in 2 studies
2 other study(ies) available for 5-(4-methoxybenzylidene)thiazolidine-2-4-dione and 2-4-thiazolidinedione
| Article | Year |
|---|---|
Synthesis and structure-activity relationship studies of 2,4-thiazolidinediones and analogous heterocycles as inhibitors of dihydrodipicolinate synthase.
Dihydrodipicolinate synthase (DHDPS), responsible for the first committed step of the diaminopimelate pathway for lysine biosynthesis, has become an attractive target for the development of new antibacterial and herbicidal agents. Herein, we report the discovery and exploration of the first inhibitors of E. coli DHDPS which have been identified from screening lead and are not based on substrates from the lysine biosynthesis pathway. Over 50 thiazolidinediones and related analogues have been prepared in order to thoroughly evaluate the structure-activity relationships against this enzyme of significant interest. Topics: Dose-Response Relationship, Drug; Enzyme Inhibitors; Escherichia coli; Heterocyclic Compounds; Hydro-Lyases; Molecular Structure; Structure-Activity Relationship; Thiazolidinediones | 2021 |
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 |