41499-21-2Relevant academic research and scientific papers
Bicyclic Picomolar OGA Inhibitors Enable Chemoproteomic Mapping of Its Endogenous Post-translational Modifications
Ashmus, Roger A.,Busmann, Jil A.,Davies, Gideon J.,Foster, Leonard J.,García Fernández, José M.,González-Cuesta, Manuel,Madden, Zarina,Males, Alexandra,Ortiz Mellet, Carmen,Proceviat, Cameron,Rogalski, Jason C.,Sidhu, Peter,Vocadlo, David J.
supporting information, p. 832 - 844 (2022/01/19)
Owing to its roles in human health and disease, the modification of nuclear, cytoplasmic, and mitochondrial proteins with O-linked N-acetylglucosamine residues (O-GlcNAc) has emerged as a topic of great interest. Despite the presence of O-GlcNAc on hundre
Application of sulfur-containing isocyanate compounds in growth inhibition of blue-green algae
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Paragraph 0042-0048; 0114-0118, (2020/04/29)
The invention relates to the application of sulfur-containing isocyanate compounds in the growth inhibition of blue-green algae. The compounds have structures as shown in a general formula I and a general formula II. In the general formula I, R1 represents a methyl group, a phenethyl group, a phenyl group, 4-methylpyridine or 3-methylpyridine. In the general formula II, M represents a carbonyl group, a methylene group and a methylene phenyl group; R3 represents hydrogen or chlorine; R4 represents oxygen, hydrogen, fluorine or chlorine; R5 represents oxygen, hydrogen, chlorine, a methyl group,fluorine, a benzene ring, bromine or a trifluoromethyl group; when R4 and R5 are oxygen, R4 and R5 are cyclized to form 1,3-dioxocyclopentene; R6 represents hydrogen, fluorine, bromine, a trifluoromethyl group, a methyl group and chlorine; and R7 represents hydrogen, a trifluoromethyl group, chlorine and bromine. The sulfur-containing isocyanate compounds with the structures as shown in the general formulas I and II provided by the invention have relatively good inhibition effect on blue-green algae, and can be used as an effective component of a blue-green algae algicide.
Differentiating Antiproliferative and Chemopreventive Modes of Activity for Electron-Deficient Aryl Isothiocyanates against Human MCF-7 Cells
Anderson, Ruthellen H.,Lensing, Cody J.,Forred, Benjamin J.,Amolins, Michael W.,Aegerter, Cassandra L.,Vitiello, Peter F.,Mays, Jared R.
, p. 1695 - 1710 (2018/08/01)
The consumption of Brassica vegetables provides beneficial effects through organic isothiocyanates (ITCs), products of the enzymatic hydrolysis of glucosinolate secondary metabolites. The ITC l-sulforaphane (l-SFN) is the principle agent in broccoli that demonstrates several modes of anticancer action. While the anticancer properties of ITCs like l-SFN have been extensively studied and l-SFN has been the subject of multiple human clinical trials, the scope of this work has largely been limited to those derivatives found in nature. Previous studies have demonstrated that structural changes in an ITC can lead to marked differences in a compound's potency to 1) inhibit the growth of cancer cells, and 2) alter cellular transcriptional profiles. This study describes the preparation of a library of non-natural aryl ITCs and the development of a bifurcated screening approach to evaluate the dose- and time-dependence on antiproliferative and chemopreventive properties against human MCF-7 breast cancer cells. Antiproliferative effects were evaluated using a commercial MTS cell viability assay. Chemopreventive properties were evaluated using an antioxidant response element (ARE)-promoted luciferase reporter assay. The results of this study have led to the identification of 1) several key structure–activity relationships and 2) lead ITCs for continued development.
Reaction of Thiocarbonyl Fluoride Generated from Difluorocarbene with Amines
Yu, Jiao,Lin, Jin-Hong,Xiao, Ji-Chang
supporting information, p. 16669 - 16673 (2017/12/07)
The reaction of thiocarbonyl fluoride, generated from difluorocarbene, with various amines under mild conditions is described. Secondary amines, primary amines, and o-phenylenediamines are converted to thiocarbamoyl fluorides, isothiocyanates, and difluoromethylthiolated heterocycles, respectively. Thiocarbamoyl fluorides were further transformed into trifluoromethylated amines by using a one-pot process. Thiocarbonyl fluoride is generated in situ and is rapidly fully converted in one pot under mild conditions; therefore, no special safety precautions are needed.
Isothiocyanates from tosyl chloride mediated decomposition of in situ generated dithiocarbamic acid salts
Wong, Rince,Dolman, Sarah J.
, p. 3969 - 3971 (2008/02/01)
(Chemical Equation Presented) A facile and general protocol for the preparation of isothiocyanates from alkyl and aryl amines is reported. This method relies on a tosyl chloride mediated decomposition of a dithiocarbamate salt that is generated in situ by treatment of an amine with carbon disulfide and triethylamine. Utilizing this protocol, we have prepared 19-alkyl- and arylisothiocyanates in moderate to excellent yield.
Bronchorelaxing compounds
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Page/Page column 16, (2010/02/13)
A compound of the general formula (I) including its pharmaceutically acceptable acid addition salts wherein A is CHR9, wherein R9 is H, C1-C6 alkyl; n is 1-3; B is CHR10, wherein R10 is H, C1-C6 alkyl; m is 1 or 2; D is O or S or optionally NR16, wherein R16 is H, C1-C6 alkyl or C2-C6 acyl; E is CR11R12 or NR13, wherein R11 and R12 are, independent of each other, H or C1-C6 alkyl, R13 is H or C1-C6 alkyl; F is C1-C18 alkyl which may be mono- or di-unsaturated and/or substituted, is useful in treating and preventing pulmonary disease characterized by bronchoconstriction. Also disclosed are pharmaceutical compositions comprising the compound and methods for their manufacture.
