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《Bioorganic & medicinal chemistry letters》2014,24(16):3802-3806
Poly(ADP-ribose) polymerase (PARP) and poly(ADP-ribose) glycohydrolase (PARG) are enzymes responsible for catalyzing the formation and degradation of poly(ADP-ribose) (PAR) polymers, respectively. Activation of PARP has been shown to be involved in cell death induced by genotoxic stimuli. On the other hand, genetic disruption of PARG also leads to increased level of cell death by accumulation of PAR. Unlike PARP, where significant medicinal effort has been expended to identify potent inhibitors, PARG has been insufficiently investigated as a molecular therapeutic target. In this study, we report the design, synthesis, and biological evaluation of phenolic hydrazide hydrazones as potent PARG inhibitors. Compounds 3d, 3e, 5d, 5e, 8a, 8b and 8c showed their ability to inhibit the catalytic activity of PARG in vitro with IC50 values of 1.0, 2.1, 3.1, 3.2, 3.1, 2.8 and 1.6 μM, respectively. 相似文献
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Violina T. Angelova Violeta Valcheva Nikolay G. Vassilev Rosen Buyukliev Georgi Momekov Ivan Dimitrov Luciano Saso Mirjana Djukic Boris Shivachev 《Bioorganic & medicinal chemistry letters》2017,27(2):223-227
This study reports the synthesis of new 2H-chromene or coumarin based acylhydrazones, which were evaluated for their in vitro antimycobacterial activity against reference strain Mycobacterium tuberculosis H37Rv and compared to the first-line antituberculosis drugs, isoniazid (INH) and ethambutol (EMB). The most active compounds 7m (MIC 0.13 μM), 7o (MIC 0.15 μM) and 7k (MIC 0.17 μM) demonstrated antimycobacterial activity at submicromolar concentration level and remarkably minimal associated cytotoxicity in the human embryonic kidney cell line HEK-293T. Structure-activity relationship for this class of compounds has been established. 相似文献
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