1373443-03-8Relevant articles and documents
NOVEL COMPOUND HAVING MALATE DEHYDROGENASE INHIBITORY ACTIVITY AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CANCER COMPRISING SAME AS ACTIVE INGREDIENT
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Paragraph 0246; 0321; 0327; 0328, (2020/02/14)
The present invention relates to a compound exhibiting inhibitory activity of at least one of malate dehydrogenases I (MDH1) and malate dehydrogenases 2 (MDH2), and a pharmaceutical composition for preventing or treating cancer comprising the same as an active ingredient. The inventors of the present invention have experimentally confirmed that the compound exhibiting the MDH1 and/or MDH2 inhibitory activity has an inhibitory effect on mitochondrial respiration in cancer cells, an excellent inhibitory effect on cancer cell growth, etc. Thus, the compound of the present invention is expected to be effectively used as a pharmaceutical composition for treating cancer.
Phenoxyacrylic derivatives and use thereof
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, (2016/10/10)
The present invention relates to a phenoxyacrylic derivative and a pharmaceutical composition comprising the same as an active ingredient for preventing or treating a nonalcoholic fatty liver disease. The compound according to the present invention has an
Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as Hypoxia-Inducible Factor (HIF) 1α inhibitors
Naik, Ravi,Won, Misun,Kim, Bo-Kyung,Xia, Yan,Choi, Hyun Kyung,Jin, Guanghai,Jung, Youngjin,Kim, Hwan Mook,Lee, Kyeong
supporting information, p. 10564 - 10571 (2013/02/22)
A series of (E)-phenoxyacrylic amide derivatives were synthesized and evaluated as hypoxia inducible factor (HIF) 1α inhibitors. The present structure-activity relationship study on this series identified the morpholinoethyl containing ester 4p as a potent inhibitor of HIF-1α under hypoxic conditions (IC50 = 0.12 μM in a cell-based HRE reporter assay) in HCT116 cells. The representative compound 4p suppressed hypoxia-induced HIF-1α accumulation and targeted gene expression in a dose-dependent manner. The effect of HIF-1α inhibition by 4p was further demonstrated by its inhibitory activity on in vitro tube formation and migration of cells, which may be valuable for development of novel therapeutics for cancer and tumor angiogenesis.