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. 2021;69(9):854-861.
doi: 10.1248/cpb.c21-00264.

2-Thioxothiazolidin-4-one Analogs as Pan-PIM Kinase Inhibitors

Yanghwan Yun  1 , Victor Sukbong Hong  1 , Seungik Jeong  1 , Hyeonseong Choo  1 , Shin Kim  2 , Jinho Lee  1
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Free article

2-Thioxothiazolidin-4-one Analogs as Pan-PIM Kinase Inhibitors

Yanghwan Yun et al. Chem Pharm Bull (Tokyo). 2021.
Free article

Abstract

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.

Keywords: cancer; inhibitor; leukemia; proviral integration site for Moloney murine leukemia virus (PIM) kinase; rhodanine.

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