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2-Thioxothiazolidin-4-one Analogs as Pan-PIM Kinase Inhibitors
Chemical & Pharmaceutical Bulletin  (IF1.645),  Pub Date : 2021-09-01, DOI: 10.1248/cpb.c21-00264
Yanghwan Yun, Victor Sukbong Hong, Seungik Jeong, Hyeonseong Choo, Shin Kim, Jinho Lee

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.

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