Bataille, Carole J. R.; Brennan, Meabh B.; Byrne, Simon; Davies, Stephen G.; Durbin, Matthew; Fedorov, Oleg; Huber, Kilian V. M.; Jones, Alan M.; Knapp, Stefan; Liu, Gu; Nadali, Anna; Quevedo, Camilo E.; Russell, Angela J.; Walker, Roderick G.; Westwood, Robert; Wynne, Graham M. published the artcile< Thiazolidine derivatives as potent and selective inhibitors of the PIM kinase family>, SDS of cas: 1003-32-3, the main research area is thiazolidine preparation serine threonine kinase inhibitor anticancer agent; Knoevenagel condensation Sukuki coupling; Anti-cancer; High throughput screen; Kinase inhibitor; PIM kinase; Thiazolidine.
The PIM family of serine/threonine kinases have become an attractive target for anti-cancer drug development, particularly for certain hematol. malignancies. Here, we describe the discovery of a series of inhibitors of the PIM kinase family using a high throughput screening strategy. Through a combination of mol. modeling and optimization studies, the intrinsic potencies and mol. properties of this series of compounds was significantly improved. An excellent pan-PIM isoform inhibition profile was observed across the series, while optimized examples show good selectivity over other kinases. Two PIM-expressing leukemic cancer cell lines, MV4-11 and K562, were employed to evaluate the in vitro anti-proliferative effects of selected inhibitors. Encouraging activities were observed for many examples, with the best example (44) giving an IC50 of 0.75 μM against the K562 cell line. These data provide a promising starting point for further development of this series as a new cancer therapy through PIM kinase inhibition.
Bioorganic & Medicinal Chemistry published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, SDS of cas: 1003-32-3.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica