116546-04-4Relevant articles and documents
A molecular approach to rationally constructing specific fluorogenic substrates for the detection of acetylcholinesterase activity in live cells, mice brains and tissues
Wu, Xiaofeng,An, Jong Min,Shang, Jizhen,Huh, Eugene,Qi, Sujie,Lee, Eunhye,Li, Haidong,Kim, Gyoungmi,Ma, Huimin,Oh, Myung Sook,Kim, Dokyoung,Yoon, Juyoung
, p. 11285 - 11292 (2020/11/04)
Acetylcholinesterase (AChE) is an extremely critical hydrolase tightly associated with neurological diseases. Currently, developing specific substrates for imaging AChE activity still remains a great challenge due to the interference from butyrylcholinesterase (BChE) and carboxylesterase (CE). Herein, we propose an approach to designing specific substrates for AChE detection by combining dimethylcarbamate choline with a self-immolative scaffold. The representative P10 can effectively eliminate the interference from CE and BChE. The high specificity of P10 has been proved via imaging AChE activity in cells. Moreover, P10 can also be used to successfully map AChE activity in different regions of a normal mouse brain, which may provide important data for AChE evaluation in clinical studies. Such a rational and effective approach can also provide a solid basis for designing probes with different properties to study AChE in biosystems and another way to design specific substrates for other enzymes. This journal is
Design and synthesis of dimethylaminomethyl-substituted curcumin derivatives/analogues: Potent antitumor and antioxidant activity, improved stability and aqueous solubility compared with curcumin
Fang, Xubin,Fang, Lei,Gou, Shaohua,Cheng, Lin
supporting information, p. 1297 - 1301 (2013/03/28)
A series of dimethylaminomethyl-substituted curcumin derivatives/analogues were designed and synthesized. All compounds effectively inhibited HepG2, SGC-7901, A549 and HCT-116 tumor cell lines proliferation in MTT assay. Particularly, compounds 2a and 3d showed much better activity than curcumin against all of the four tumor cell lines. Antioxidant test revealed that these compounds had higher free radical scavenging activity than curcumin towards both DPPH and galvinoxyl radicals. Furthermore, the aqueous solubility and stability of the target compounds were also significantly improved compared with curcumin.
Synthesis, spectroscopic characterization and chemical reactions of stable o-QM on solid phase
Zanaletti, Riccardo,Freccero, Mauro
, p. 1908 - 1909 (2007/10/03)
A novel approach towards quinone methides stabilization has been achieved by anchoring the reactive o-QM intermediate on solid phase (RTHP). The reactivity and selectivity of supported o-QM towards N and S centered nucleophiles have been explored.