1000339-30-9Relevant articles and documents
2-thioxothiazolidin-4-one analogs as pan-pim kinase inhibitors
Yun, Yanghwan,Hong, Victor Sukbong,Jeong, Seungik,Choo, Hyeonseong,Kim, Shin,Lee, Jinho
, p. 854 - 861 (2021/09/06)
Proviral integration site for Moloney murine leukemia virus (PIM) kinases are proto-oncogenic kinases involved in the regulation of several cellular processes. PIM kinases are promising targets for new drug development because they play a major role in many cancer-specific pathways, such as survival, apoptosis, proliferation, cell cycle regulation, and migration. Here, 2-thioxothiazolidin-4-one derivatives were synthesized and evaluated as potent pan-PIM kinase inhibitors. Optimized compounds showed single-digit nanomolar IC50 values against all three PIM kinases with high selectivity over 14 other kinases. Compound 17 inhibited the growth of Molm-16 cell lines (EC50 = 14 nM) and modulated the expression of pBAD and p4EBP1 in a dose-dependent manner.
Selective mono-amination of dichlorodiazines
Sengmany, Stéphane,Lebre, Julie,Le Gall, Ewan,Léonel, Eric
, p. 4859 - 4867 (2015/08/03)
A mild, easy-to-perform, and versatile method for the formation of aminochlorodiazines from reaction of several types of dichlorodiazines (i.e., pyridazines, pyrimidines, and pyrazines) with primary or secondary amines in ethanol in the presence of trieth