D9 是一种有效的选择性硫氧还蛋白还原酶 (TrxR) 抑制剂,EC50 为 2.8 nM。 D9 具有在体外和体内抑制肿瘤增殖的能力。
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Potent thioredoxin reductase (TrxR) inhibitor (EC50 = 2.8 nM, IC50 = 0.03 and 0.1 μM in MCF-7 cells and HT-29 cells, respectively). Highly stable in vivo; exhibits no significant ligand exchange with albumin. Inhibits tumor proliferation in vitro and in vivo by inducing cell death. Selectively kills cancer cells.
Zhang et al (2014) Synthesis and molecular recognition studies on small-molecule inhibitors for thioredoxin reductase. J.Med.Chem. 57 8132 PMID:25249032 |Lin et al (2015) pH-sensitive polymeric nanoparticles with gold(I) compound payloads synergistically induce cancer cell death through modulation of autophagy. Mol.Pharm. 12 2869 PMID:26101892
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