426829-52-9Relevant 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.
NOVEL NITROGEN-CONTAINING AROMATIC HETEROCYCLIC COMPOUND
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Paragraph 0153, (2018/10/15)
A compound represented by general formula [1] wherein X represents N or the like, Y represents CH or the like; RA represents a cycloalkyl group which may be substituted or the like, R1 represents an alkyl group or the like, R2 represents an alkyl group which may be substituted or the like, R3 represents a hydrogen atom or an alkyl group, or a pharmaceutically acceptable salt thereof has an inhibitory activity on aldosterone synthetase, and is useful as a prophylactic and/or therapeutic agent for various diseases or symptoms associated with aldosterone.
Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases
Nishiguchi, Gisele A.,Atallah, Gordana,Bellamacina, Cornelia,Burger, Matthew T.,Ding, Yu,Feucht, Paul H.,Garcia, Pablo D.,Han, Wooseok,Klivansky, Liana,Lindvall, Mika
supporting information; experimental part, p. 6366 - 6369 (2011/12/02)
A series of novel 3,5-disubstituted indole derivatives as potent and selective inhibitors of all three members of the Pim kinase family is described. High throughput screen identified a pan-Pim kinase inhibitor with a promiscuous scaffold. Guided by struc