80180-46-7Relevant academic research and scientific papers
Nivel 1,2-Dithiins: Synthesis, Molecular Modeling Studies, and Antifungal Activity
Bierer, Donald E.,Dener, Jeffrey M.,Dubenko, Larisa G.,Gerber, R. Eric,Litvak, Joane,et al.
, p. 2628 - 2648 (1995)
The first structure-activity study involving the 1,2-dithiin class of compounds (1,2-dithiacyclohexadienes) is herein reported.A series of 3,6-disubstituted 1,2-dithiins was synthesized from dithiins 1d and 1e and evaluated as antifungal agents.A new and versatile synthesis of dithiins 1d and 1e is reported which is amenable to scale-up at the kilogram level.The novelty of the process derives from the use of β-mercaptopropionitrile as the thiophile, relying on a β-elimination strategy and subsequent oxidation to create the 1,2-dithiin ring.Optimal geometries of dithiins 1d, 18i, and 45 and model dithiin 61 were determined by molecular mechanics and Hartree-Fock molecular orbital calculations.Two possible mechanisms of action are presented for the 1,2-dithiin class of compounds to explain their observed antifungal activities against Candida albicans, Cryptococcus neoformans, and Aspergillus fumigatus.
COMPOUNDS COMPRISING CLEAVABLE LINKER AND USES THEREOF
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Page/Page column 148, (2020/09/03)
Provided are a compound including a cleavable linker, a use thereof, and an intermediate compound for preparing the same, and more particularly, the compound including a cleavable linker of the present invention may include an active agent (for example, a drug, a toxin, a ligand, a probe for detection, etc.) having a specific function or activity, a -S(=0)(=N-)- functional group which is capable of selectively releasing the active agent, and a functional group which triggers a chemical reaction, a physicochemical reaction and/or a biological reaction by external stimulation, and may further include a ligand (for example, oligopeptide, polypeptide, antibody, etc.) having binding specificity for a desired target receptor.
COMPOUNDS COMPRISING CLEAVABLE LINKER AND USES THEREOF
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Page/Page column 144, (2019/01/21)
Provided are a compound including a cleavable linker, a use thereof, and an intermediate compound for preparing the same, and more particularly, the compound including a cleavable linker of the present invention may include an active agent (for example, a drug, a toxin, a ligand, a probe for detection, etc.) having a specific function or activity, a SO2 functional group which is capable of selectively releasing the active agent, and a functional group which triggers a chemical reaction, a physicochemical reaction and/or a biological reaction by external stimulation, and may further include a ligand (for example, oligopeptide, polypeptide, antibody, etc.) having binding specificity for a desired target receptor.
A series of F-Element chelators; diaza crown ethers functionalized with catecholate binding substituents
Stein, Benjamin W.,Cary, Samantha K.,Berg, John M.,Birnbaum, Eva R.,Kozimor, Stosh A.,Mocko, Veronika,Scott, Brian L.
, p. 170 - 179 (2018/01/01)
Reported here is the preparation of azacrown ethers functionalized with catechol groups. The synthetic approach was (1st) novel in that it made use of the Mannich reaction and (2nd) valuable in that it provided an improved synthesis (in terms of practical
AZOARYLS AS REVERSIBLY MODULATABLE TUBULIN INHIBITORS
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Page/Page column 64, (2015/11/23)
The invention concerns a new class of tubulin polymerisation inhibitors and their applications in research and medicine, notably in chemotherapy. The invention proposes new azoaryl derivatives of formula (I): as defined in Claim 1, which may be fully reve
Microwave-assisted protection of phenols as tert-butyldimethylsilyl (TBDMS) ethers under solvent-free conditions
Bastos, Erick L.,Ciscato, Luiz F. M. L.,Baader, Wilhelm J.
, p. 1501 - 1509 (2007/10/03)
A facile, time-saving procedure to protect phenols with tert-butyldimethylsilyl chloride using imidazole as catalyst under solvent-free conditions is described. Several phenolic compounds with different substitution patterns can be silylated in high yield
