- Design of OFF/ON fluorescent thiol probes based on coumarin fluorophore
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This paper presents a series of first- and second-generation click-modified coumarin-based fluorescent probes for thiols. These molecules demonstrate high turn-on fluorescent response and good selectivity towards aromatic thiols over other relevant reactive sulfur species, reactive oxygen species and common nucleophiles. Moreover, probe 1a can detect thiols in the reduced rabbit plasma sample. Therefore, this approach provides a particularly impressive tool for detecting thiol in biological systems. Science China Press and Springer-Verlag Berlin Heidelberg 2012.
- Sun, Wei,Li, Jing,Li, Wenhua,Su, Lijuan,Du, Lupei,Li, Minyong
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- TRICYCLIC HETEROAROMATIC COMPOUNDS AS ALPHA-SYNUCLEIN LIGANDS
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Derivatives of phenothiazine, phenoxazine, and phenazine compounds and their use as α-synuclein ligands are described. Also described are methods of using these compounds and their radiolabeled analogs for the detection, monitoring, and treatment of synucleinopathies, including Parkinson's disease.
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Paragraph 0134
(2013/12/04)
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- A benzothiazole-based fluorescent probe for thiol bioimaging
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This study reports a benzothiazole-based fluorescent probe with simple structure for thiols. This probe exhibited high on/off signal ratios and good selectivity toward thiols over other analytes, and was successfully applied to the imaging of thiols in living cells.
- Sun, Wei,Li, Wenhua,Li, Jing,Zhang, Jian,Du, Lupei,Li, Minyong
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p. 2332 - 2335
(2012/07/14)
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- Synthesis and in vitro evaluation of α-synuclein ligands
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Accumulation of misfolded α-synuclein in Lewy bodies and Lewy neurites is the pathological hallmark of Parkinson's disease (PD). To identify ligands having high binding potency toward aggregated α-synuclein, we synthesized a series of phenothiazine derivatives and assessed their binding affinity to recombinant α-synuclein fibrils using a fluorescent thioflavin T competition assay. Among 16 new analogues, the in vitro data suggest that compound 11b has high affinity to α-synuclein fibrils (Ki = 32.10 ± 1.25 nM) and compounds 11d, 16a and16b have moderate affinity to α-synuclein fibrils (Ki ≈ 50-100 nM). Further optimization of the structure of these analogues may yield compounds with high affinity and selectivity for aggregated α-synuclein.
- Yu, Lihai,Cui, Jinquan,Padakanti, Prashanth K.,Engel, Laura,Bagchi, Devika P.,Kotzbauer, Paul T.,Tu, Zhude
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experimental part
p. 4625 - 4634
(2012/09/05)
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- N-Acylaminophenothiazines: Neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease
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We have previously reported the multifunctional profile of N-(3-chloro-10H-phenothiazin-10-yl)-3-(dimethylamino)propanamide (1) as an effective neuroprotectant and selective butyrylcholinesterase inhibitor. In this paper, we have developed a series of N-acylaminophenothiazines obtained from our compound library or newly synthesised. At micro- and sub-micromolar concentrations, these compounds selectively inhibited butyrylcholinesterase (BuChE), protected neurons against damage caused by both exogenous and mitochondrial free radicals, showed low toxicity, and could penetrate into the CNS. In addition, N-(3-chloro-10H-phenothiazin-10-yl)-2-(pyrrolidin-1-yl) acetamide (11) modulated the cytosolic calcium concentration and protected human neuroblastoma cells against several toxics, such as calcium overload induced by an l-type Ca2+-channel agonist, tau-hyperphosphorylation induced by okadaic acid and Aβ peptide.
- González-Mu?oz, Gema C.,Arce, Mariana P.,López, Beatriz,Pérez, Concepción,Romero, Alejandro,Barrio, Laura Del,Martín-De-Saavedra, María Dolores,Egea, Javier,León, Rafael,Villarroya, Mercedes,López, Manuela G.,García, Antonio G.,Conde, Santiago,Rodríguez-Franco, María Isabel
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body text
p. 2224 - 2235
(2011/06/22)
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- Intramolecular Catalysis. Part 7. The Smiles Rearrangement of Substituted 2-Hydroxy-2'-nitro- and -2',4'-Dinitro-diphenyl Sulphones, as well as 2-Amino-2',4'-dinitrodiphenyl Sulphide, 2--3-nitropyridine and 2-Hydroxy-2',4'-dinitrodiph
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Rate coefficients have been measured for the Smiles rearrangement of a series of 4- and 5-substituted 2-hydroxy-2'-nitrodiphenyl sulphones in 70percent (v/v) dioxane-water at 60.0 deg C, and for three substrates at several temperatures.The activation para
- Bowden, Keith,Williams, Philip R.
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p. 215 - 224
(2007/10/02)
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