642459-26-5Relevant 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.
PYRAZINE DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS
-
Page/Page column 22, (2009/04/25)
This invention relates to novel pyrazine derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with t