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1,3, 4‐Oxadiazole ‐2( 3 H )‐thione Analogs as PIM Kinase Inhibitors
Author(s) -
Hong Victor Sukbong,
Jeong Seungik,
Yun Yanghwan,
Choo Hyeonseong,
Won Jongin,
Lee Jinho
Publication year - 2020
Publication title -
bulletin of the korean chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.237
H-Index - 59
ISSN - 1229-5949
DOI - 10.1002/bkcs.12101
Subject(s) - kinase , chemistry , biochemistry , cancer research , microbiology and biotechnology , biology
Proviral integration site for moloney murine leukemia virus (PIM) kinases are highly expressed in hematological cancers. They phosphorylate downstream substrates that contribute to tumor growth and survival. Therefore, a potent inhibitor of PIM kinases is expected to be effective at treating hematological cancers. In the present study, several indole derivatives of 1,3,4‐oxadiazole‐2(3 H )‐thione were synthesized and evaluated as PIM kinase inhibitors. Structure–activity relationship studies yielded potent inhibitors of all three PIM kinases in the single‐digit to low double‐digit nanomolar IC 50 range. Kinase profiling of a representative compound showed high selectivity among 15 other kinases.