88999-92-2Relevant academic research and scientific papers
Decarboxylative Thiolation of Redox-Active Esters to Thioesters by Merging Photoredox and Copper Catalysis
Cao, Tianpeng,Liao, Saihu,Nie, Xingliang,Xu, Ruting,Xu, Tianxiao,Yang, Mingcheng
supporting information, p. 3692 - 3696 (2020/04/21)
Thioesters and related thiols are critically important to biological systems and also widely employed in the synthesis of pharmaceutically important molecules and polymeric materials. However, known synthetic methods often suffer from the disadvantage of
The swallow-tailed side chain containing sulfide six benzene and cronene compound and its preparation method
-
Paragraph 0075; 0076; 0077; 0078, (2017/06/30)
The invention relates to a hexabenzocoronene compound containing thioether in the dovetail-like side-chain and a preparation method thereof. The structural general formula of the compound is described in the specification, and in the formula, R is a dovet
Inhibition of monoamine oxidase by 8-[(phenylethyl)sulfanyl]caffeine analogues
Mostert, Samantha,Mentz, Wayne,Petzer, Anél,Bergh, Jacobus J.,Petzer, Jacobus P.
, p. 7040 - 7050 (2013/01/15)
In a previous study we have investigated the monoamine oxidase (MAO) inhibitory properties of a series of 8-sulfanylcaffeine analogues. Among the compounds studied, 8-[(phenylethyl)sulfanyl]caffeine (IC50 = 0.223 μM) was found to be a particularly potent inhibitor of the type B MAO isoform. In an attempt to discover potent MAO inhibitors and to further examine the structure-activity relationships (SAR) of MAO inhibition by 8-sulfanylcaffeine analogues, in the present study a series of 8-[(phenylethyl)sulfanyl]caffeine analogues were synthesized and evaluated as inhibitors of human MAO-A and -B. The results document that substitution on C3 and C4 of the phenyl ring with alkyl groups and halogens yields 8-[(phenylethyl)sulfanyl]caffeine analogues which are potent and selective MAO-B inhibitors with IC50 values ranging from 0.017 to 0.125 μM. The MAO inhibitory properties of a series of 8-sulfinylcaffeine analogues were also examined. The results show that, compared to the corresponding 8-sulfanylcaffeine analogues, the 8-sulfinylcaffeins are weaker MAO-B inhibitors. Both the 8-sulfanylcaffeine and 8-sulfinylcaffeine analogues were found to be weak MAO-A inhibitors. This study also reports the MAO inhibition properties of selected 8-[(phenylpropyl)sulfanyl]caffeine analogues.
Synthesis of radioiodine-labeled 2-phenylethyl 1-thio-β-D-galactopyranoside for imaging of LacZ gene expression
Choi, Joon Hun,Choe, Yearn Seong,Lee, Kyung-Han,Choi, Yong,Kim, Sang Eun,Kim, Byung-Tae
, p. 29 - 34 (2007/10/03)
A potent inhibitor of β-galactosidase (EC 3.2.1.23), 2-phenylethyl 1-thio-β-D-galactopyranoside (PETG), was radioiodinated for noninvasive imaging of LacZ gene expression. In order to introduce radioiodine to the phenyl ring of PETG, 2-(4-bromophenyl)ethanethiol was prepared and attached to the C-1 position of β-D-galactose pentaacetate under conditions that resulted in the exclusive formation of the β anomer. The bromo group of PETG was converted to the tributylstannyl group where radioiododemetallation was carried out. Radioiodine-labeled PETG tetraacetate was purified by HPLC, which can be used as a prodrug for biological evaluation or hydrolyzed to 2-(4-[123I/125I]iodophenyl)ethyl 1-thio-β-D-galactopyranoside ([123I/125I]7) under basic conditions. The resulting radioiodine-labeled PETG was obtained in overall 62% radiochemical yield (decay-corrected) and with specific activity of 46-74 GBq/μmol.
Uracil derivatives. IV. Growth-inhibitory activity against L-1210 cells of orotic acid derivatives and synthesis of 1-(β-D-ribofuranosyl)furo[3,4-d]pyrimidine-2,4,7(1H,3H,5H)-trione
Okada,Nakano,Miyake
, p. 3074 - 3083 (2007/10/02)
5-(Substituted thiomethyl)-6-carbamoyluracils (IIIb-h) and 5-(substituted thiomethyl)-uracils (Va-h) were prepared and their ability to inhibit the growth of L-1210 cells in vitro was examined. The reaction of silylated furo[3,4-d]pyrimidine-2,4,7(1H,3H,5
