- Tunable Heteroaromatic Sulfones Enhance in-Cell Cysteine Profiling
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Heteroaromatic sulfones react with cysteine via nucleophilic aromatic substitution, providing a mechanistically selective and irreversible scaffold for cysteine conjugation. Here we evaluate a library of heteroaromatic sulfides with different oxidation st
- Motiwala, Hashim F.,Kuo, Yu-Hsuan,Stinger, Brittany L.,Palfey, Bruce A.,Martin, Brent R.
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supporting information
p. 1801 - 1810
(2020/02/04)
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- Design, synthesis and evaluation of benzothiazole derivatives as multifunctional agents
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Oxidative stress is the product or aetiology of various multifactorial diseases; on the other hand, the development of multifunctional compounds is a recognized strategy for the control of complex diseases. To this end, a series of benzothiazole derivatives was synthesized and evaluated for their multifunctional effectiveness as antioxidant, sunscreen (filter), antifungal and antiproliferative agents. Compounds were easily synthesized via condensation reaction between 2-aminothiophenols and different benzaldehydes. SAR study, particularly in position 2 and 6 of benzothiazoles, led to the identification of 4g and 4k as very interesting potential compounds for the design of multifunctional drugs. In particular, compound 4g is the best blocker of hERG potassium channels expressed in HEK 293 cells exhibiting 60.32percent inhibition with IC50 = 4.79 μM.
- Andreotti, Elisa,Baldisserotto, Anna,Balzarini, Jan,Buzzi, Raissa,Dissette, Valeria,Djuidje, Ernestine Nicaise,Liekens, Sandra,Manfredini, Stefano,Sciabica, Sabrina,Serra, Elena,Vertuani, Silvia
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- Synthesis and evaluation of18F-labeled 2-phenylbenzothiazoles as positron emission tomography imaging agents for amyloid plaques in alzheimer's disease
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Imaging agents targeting amyloid β(Aβ) may be useful for early diagnosis and follow-up of treatment of patients with Alzheimer's disease (AD). Three of five tested 2-(4′-fluorophenyl)-1,3-benzothiazoles displayed high binding affinities for Aβ plaques in
- Serdons, Kim,Terwinghe, Christelle,Vermaelen, Peter,Van Laere, Koen,Kung, Hank,Mortelmans, Luc,Bormans, Guy,Verbruggen, Alfons
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experimental part
p. 1428 - 1437
(2009/12/26)
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