gw-5074 has been researched along with Leukemia--Myelogenous--Chronic--BCR-ABL-Positive* in 1 studies
1 other study(ies) available for gw-5074 and Leukemia--Myelogenous--Chronic--BCR-ABL-Positive
| Article | Year |
|---|---|
Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity.
Breakpoint cluster region-Abelson (Bcr-Abl) kinase is a key driver in the pathophysiology of chronic myelogenous leukemia (CML). Broadening the chemical diversity of Bcr-Abl kinase inhibitors with novel chemical entities possessing favorable target potency and cellular efficacy is a current medical demand for CML treatment. In this respect, a new series of ethynyl bearing 3-aminoindazole based Bcr-Abl inhibitors has been designed, synthesized, and biologically evaluated. The target compounds were designed based on introducing the key structural features of ponatinib, alkyne spacer and diarylamide, into the previously reported indazole II to improve its Bcr-Abl inhibitory activity and overcome its poor cellular potency. All target compounds elicited potent activity against Bcr-Abl Topics: Amination; Antineoplastic Agents; Cell Proliferation; Drug Design; Fusion Proteins, bcr-abl; Humans; Indazoles; K562 Cells; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Molecular Docking Simulation; Protein Kinase Inhibitors | 2020 |