Juen, Ludovic published the artcileNew Inhibitor Targeting Signal Transducer and Activator of Transcription 5 (STAT5) Signaling in Myeloid Leukemias, COA of Formula: C17H27BN2O4S, the publication is Journal of Medicinal Chemistry (2017), 60(14), 6119-6136, database is CAplus and MEDLINE.
Signal Transducer and Activator of Transcription 5 (STAT5) are crucial effectors of tyrosine kinase oncogenes in myeloid leukemias. Inhibition of STAT5 would contribute to reducing the survival of leukemic cells and also tackling their chemoresistance. In a first screening experiment, the authors identified hit 13 (I) as able to inhibit STAT5 phosphorylation and leukemic cell growth. The synthesis of 18 analogs of 13 allowed the authors to identify one compound, 17f (II), as having the most potent antileukemic effect. Compound 17f inhibited the growth of acute and chronic myeloid leukemia cells and phosphorylation and transcriptional activity of STAT5. Importantly, 17f had minimal effects on bone marrow stromal cells that play vital functions in the microenvironment of hematopoietic and leukemic cells. The authors also demonstrated that 17f inhibits STAT5 but not STAT3, AKT or Erk1/2 phosphorylation. These results suggest that 17f might be a new lead mol. targeting STAT5 signaling in myeloid leukemias.
Journal of Medicinal Chemistry published new progress about 914610-39-2. 914610-39-2 belongs to piperazines, auxiliary class Piperazine,Boronic acid and ester,Sulfamide,Benzene,Piperazine,Boronate Esters,Boronic acid and ester,, name is 1-Methyl-4-((4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)sulfonyl)piperazine, and the molecular formula is C17H27BN2O4S, COA of Formula: C17H27BN2O4S.
Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics