- Maleimidation of dextran and the application in designing a dextran-camptothecin conjugate
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Camptothecin analogs, as commonly used chemotherapy drugs, usually have poor water solubility which has limited their use in the clinic. In order to improve the water-solubility of camptothecin, a new dextran derivative Dex-Mal was synthesized and used in
- Zhu, Qiwen,Bao, Bin,Zhang, Qiumeng,Yu, Jiahui,Lu, Wei
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Read Online
- Supramolecular chirality of coordination polymers of Ag+ with a chiral thiol ligand that bears a β-turn structure
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We report coordination polymers forming from Ag+ and a chiral thiol ligand that bears a β-turn structure, exhibiting supramolecular chirality showing both the majority rules effect (MRE) and the racemate rules effect (RRE).
- Yuan, Yuan,Xiao, Yu-Wei,Yan, Xiao-Sheng,Wu, Si-Xian,Luo, Huan,Lin, Jian-Bin,Li, Zhao,Jiang, Yun-Bao
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Read Online
- PROTECTED FUMARIC ACID-BASED METABOLITES FOR THE TREATMENT OF AUTOIMMUNE DISEASES
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The present invention provides novel cell-permeable fumarate acyl mercaptoethylamines (FAMs) which have cellular effects including induction of Nrf2 and inhibition of the NFkB pathway. These compounds have utility in medicine including their use in treatment of diseases such as Multiple sclerosis, Non-alcoholic Steatohepatitis, Psoriasis, Inflammatory Arthritis, Inflammatory Bowel Disease, Asthma, Chronic Obstructive Pulmonary Disease, Cancer, Parkinson's Disease, Alzheimer's Disease, Huntington's Disease and Amyotrophic Lateral Sclerosis.
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Page/Page column 34; 35; 36
(2017/08/01)
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- Carvacrol codrugs: A new approach in the antimicrobial plan
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Objective: The increasing prevalence of antibiotic-resistant bacterial infections led to identify alternative strategies for a novel therapeutic approach. In this study, we synthesized ten carvacrol codrugs - obtained linking the carvacrol hydroxyl group
- Cacciatore, Ivana,Di Giulio, Mara,Fornasari, Erika,Di Stefano, Antonio,Cerasa, Laura Serafina,Marinelli, Lisa,Turkez, Hasan,Di Campli, Emanuela,Di Bartolomeo, Soraya,Robuffo, Iole,Cellini, Luigina
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- Substrate-initiated synthesis of cell-penetrating poly(disulfide)s
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Lessons from surface-initiated polymerization are applied to grow cell-penetrating poly(disulfide)s directly on substrates of free choice. Reductive depolymerization after cellular uptake should then release the native substrates and minimize toxicity. In the presence of thiolated substrates, propagators containing a strained disulfide from asparagusic or, preferably, lipoic acid and a guanidinium cation polymerize into poly(disulfide)s in less than 5 min at room temperature at pH 7. Substrate-initiated polymerization of cationic poly(disulfide)s and their depolymerization with dithiothreitol causes the appearance and disappearance of transport activity in fluorogenic vesicles. The same process is further characterized by gel-permeation chromatography and fluorescence resonance energy transfer.
- Bang, Eun-Kyoung,Gasparini, Giulio,Molinard, Guillaume,Roux, Aurélien,Sakai, Naomi,Matile, Stefan
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supporting information
p. 2088 - 2091
(2013/04/10)
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- The design, synthesis and photochemical study of a biomimetic cyclodextrin model of Photoactive Yellow Protein (PYP)
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The design, synthesis and study of the photophysical and photochemical properties of the first biomimetic cyclodextrin (CD) model of photoactive yellow protein (PYP) are described. This model bears a deprotonated trans-p-coumaric acid chromophore, covalently linked via a cysteine moiety to a permethylated 6-monoamino β-CD. NMR and UV/Visible spectroscopy studies showed the formation of strong self-inclusion complexes in water at basic pH. Steady-state photolysis demonstrated that, unlike the free chromophore in solution, excitation of the model molecule leads to the formation of a photoproduct identified as the cis isomer by NMR spectroscopy. These observations provide evidence that the restricted CD cavity offers a promising framework for the design of biomimetic models of the PYP hydrophobic pocket.
- Loukou, Christina,Changenet-Barret, Pascale,Rager, Marie-Noelle,Plaza, Pascal,Martin, Monique M.,Mallet, Jean-Maurice
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supporting information; experimental part
p. 2209 - 2218
(2011/05/08)
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- A magnetic biomimetic nanocatalyst for cleaving phosphoester and carboxylic ester bonds under mild conditions
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As a result of the unique surface structure of nanospheres, Asp and His residues supported on a 12 nm maghemite nanoparticle worked collaboratively as a biomimetic nanocatalyst for hydrolyzing paraoxon (phosphoester) and 4-nitrophenyl acetate (carboxylic ester) in Milli-Q water (pH 7.0) at 37 °C, without employing extremes of pH or heavy metals. Our nanocatalyst could be facilely recovered via magnetic concentration. The isolated catalyst exhibited long-term stability, showing no significant loss of its catalytic activity for repeated uses after 3 months.
- Zheng, Yan,Duanmu, Chuansong,Gao, Yong
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p. 3215 - 3217
(2007/10/03)
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- Cobalt assisted cleavage of S-S bonds and a base-free synthesis of mercapturic acids
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Base free transformation of PhSSPh to sulfides, PhSR (R = alkyl, benzyl, allyl, acyl) and N-acetyl-L-cystine to mercapturic acids [AcNHCH(COOH)CH2SR, R = alkyl, benzyl, allyl, acyl] have been achieved using Zn/cat. CoCl2/organic halide in MeCN at room temperature.
- Chowdhury, Shantanu,Roy, Sujit
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p. 2149 - 2152
(2007/10/03)
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- A convenient synthesis of S-[(2R)-2-acetamido-3-(hexadecyloxy)propyl] 2-(trimethylammonio)ethyl thiophosphate, a new amido-thiophosphate analog of PAF
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The naturally configurated S-[(2R)-2-acetamido-3-(hexadecyloxy)propyl] 2-(trimethylammonio)ethyl thiophosphate (5), a new amido-thiophosphate analog of the Platelet Activating Factor (PAF), was obtained in a seven-step reaction sequence by starting from N
- Mlotkowska, Barbara,Poscik, Adam
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p. 841 - 843
(2007/10/03)
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