3959-23-7

Usage

Uses

(Phenylsulfonyl)acetic acid is used as pharmaceutical intermediates.

InChI:InChI=1/C8H8O4S/c9-8(10)6-13(11,12)7-4-2-1-3-5-7/h1-5H,6H2,(H,9,10)

Upstream product

• 109-72-8 n-butyllithium 
• 60-29-7 diethyl ether 
• 3112-85-4 methylphenylsulfonate 
• 20611-21-6 2-(phenylsulfonyl)ethanol 
• 5296-64-0 allyl phenyl thioether 
• 64-19-7 acetic acid 
• 79-11-8 chloroacetic acid 
• 618-41-7 Benzenesulfinic acid 
• 7605-28-9 2-(phenylsulfonyl)acetonitrile 
• 34097-60-4 methyl benzenesulfonylacetate 
• 7664-93-9 sulfuric acid 
• 103-04-8 (phenylthio)acetic acid 
• 71560-75-3 1,3-bis(benzenesulfonyl)propan-2-one 
• 93249-29-7 benzenesulfonylacetyl-urea 

Downstream Products

• 129120-32-7 (E)-4-(2-(phenylsulfonyl)vinyl)pyridine 
• 7605-30-3 ethyl 2-phenylsulfonylacetate 
• 3112-85-4 methylphenylsulfonate 
• 19169-90-5 bromomethylphenylsulfone 
• 16003-66-0 ((dibromomethyl)sulfonyl)benzene 
• 31540-74-6 dichloromethyl phenyl sulfone 
• 20018-08-0 diiodomethyl-phenyl sulfone 
• 72263-17-3 phenylsulfonylacetic acid chloride 
• 3937-95-9 3-Nitrophenylsulfonylessigsaeure 
• 41173-24-4 (E)-1-chloro-2-[2-(phenylsulfonyl)vinyl]benzene 
• 102313-03-1 (E)-1-hydroxyl-4-(2-(phenylsulfonyl)vinyl)benzene 
• 171743-15-0 (E)-1-methoxy-4-[2-(4-methylbenzene)sulfonylvinyl]benzene 
• 87891-80-3 (E)-4-[2-(phenylsulfonyl)vinyl]anisole 
• 108474-86-8 (E)-1,2-dichloro-4-(2-(phenylsulfonyl)vinyl)benzene 

Relevant academic research and scientific papers

Discovery of β-carboline-(phenylsulfonyl)furoxan hybrids as potential anti-breast cancer agents

The cytotoxicity properties of the β-carboline alkaloids have been broadly investigated. However, the potential application of β-carbolines was hindered due to the moderate activity in cancer. In the present study, thirty β-carboline-(phenylsulfonyl)furoxan hybrids (11a–j, 12a–j and 13a–j) were designed and synthesized through esterification and amidation reaction strategy, and their inhibitory activities against the human breast cancer cell lines MCF-7 and MDA-MB-231 were evaluated by CCK-8 assay. Biological evaluation presented that the most promising amide derivative 13h, substituted with p-methoxyphenyl group at position 1, generated high concentration of NO and evidently depressed the MCF-7 (IC50 = 0.89 μM) and MDA-MB-231 (IC50 = 0.62 μM) cells proliferation. Particularly, the wound healing and transwell assays demonstrated that 13h significantly inhibited the migration and invasion of MDA-MB-231cells. Furthermore, the preliminary mechanisms studies indicated that 13h induced G2/M phase arrest and apoptosis possibly causing by ROS accumulation and ROS-mediated DNA damage. Based on these considerations, 13h may be a promising antimetastatic agent for breast cancer, which is noteworthy for further exploration.

Chromone 3-position nitric oxide donor derivative as well as preparation method and application thereof

The invention relates to the fields of natural medicines and medicinal chemistry, and relates to a preparation method of a series of chromone 3-position nitric oxide donor derivatives with antitumor activity and a new application of the chromone 3-position nitric oxide donor derivatives in preparation of antitumor medicines. The chromone 3-position nitric oxide donor derivative and the pharmaceutically acceptable salt thereof are shown as a general formula I in the specification. Wherein R and R1 are described in the claims and the specification.

Chromone 3-piperazine linked furazan derivative as well as preparation method and application thereof

The invention relates to the fields of natural medicines and medicinal chemistry, and relates to a preparation method of a series of chromone 3-piperazine linked furazan derivatives with antitumor activity and a new application of the chromone 3-piperazine linked furazan derivatives in preparation of antitumor medicines. The chromone 3-piperazine linked furazan derivative and the pharmaceutically acceptable salt thereof disclosed by the invention are as shown in a general formula I in the specification. Wherein R is described in the claims and the specification.

Chromone 2-position nitric oxide donor derivative as well as preparation method and application thereof

The invention relates to the fields of natural medicines and medicinal chemistry, and relates to a preparation method of a series of chromone 2-position nitric oxide donor derivatives with antitumor activity and a new application of the chromone 2-position nitric oxide donor derivatives in preparation of antitumor medicines. The chromone 2-position nitric oxide donor derivative and the pharmaceutically acceptable salt thereof are shown as a general formula I in the specification. Wherein R and R1 are described in the claims and the specification.

Chromone 2-piperazine linked furazan derivative as well as preparation method and application thereof

The invention relates to the fields of natural medicines and medicinal chemistry, and relates to a preparation method of a series of chromone 2-piperazine linked furazan derivatives with antitumor activity and a new application of the chromone 2-piperazine linked furazan derivatives in preparation of antitumor medicines. The chromone 2-piperazine linked furazan derivative and the pharmaceutically acceptable salt thereof disclosed by the invention are as shown in a general formula I in the specification. Wherein R is described in the claims and the specification.

Evaluation of novel paclitaxel-loaded NO-donating polymeric micelles for an improved therapy for gastroenteric tumor

This study reports the design and synthesis of NO-donating polymer to generate biodegradable polymeric micelle containing paclitaxel (NO/PTX) as a nanomedicine delivery system aimed to enhance the solubility and anti-cancer activity of paclitaxel (PTX). NO/PTX showed greater NO-releasing performance than nitroglycerin, displaying excellent tolerance in KM mice, and exhibited a two-fold stronger antiproliferative activity than PTXin vitroagainst HCT116, SW480, and SGC-7901 cell lines.In vivotumor growth inhibition assay results indicated that NO/PTX displayed lightly stronger activities against tumor growth than PTX at a dose of 10 mg kg?1, while the anti-tumor effect of NO/PTX was significantly improved than that of PTX and Genexol-PM groups at a dose of 15 mg kg?1(the inhibition rate: 67%vs.53% and 41%). In addition, NO/PTX showed an improved area under the plasma concentration-time curve and drug deposition in tumors in comparison to PTX. Wound healing assay and western blot analysis of EMT-related markers suggested that NO/PTX could inhibit the potential of HCT116 migration. Western blot analysis also demonstrated that NO/PTX dampened efflux activity of P-gp and up-regulated apoptosis-related proteins. Overall, these promising results suggested that the synergism between PTX and NO-donating micelles could contribute to the potent anti-cancer activity of NO/PTX.

COMPOSITES, METHODS AND USES THEREOF

The present invention relates, in general terms, to methods of catalysing a reaction, including the steps of contacting a chemical entity comprising a sulphide moiety with a composite and an oxidant. The composite acts as a heterogeneous catalyst to oxidise the sulphide moiety. The present invention also relates to composites, methods of synthesising the composites and its use as a catalyst thereof.

Antiproliferative chromone derivatives induce K562 cell death through endogenous and exogenous pathways

A series of furoxan derivatives of chromone were prepared. The antiproliferative activities were tested against five cancer cell lines HepG2, MCF-7, HCT-116, B16, and K562, and two normal human cell lines L-02 and PBMCs. Among them, compound 15a exhibited the most potent antiproliferative activity. It was also found 15a produced more than 8 μM of NO at the peak time of 45 min by Griess assay. Generally, antiproliferative activity is positively related to NO release to some extent. Further in-depth studies on apoptosis-related mechanisms showed that 15a caused S-phase cell cycle arrest in a concentration-dependent manner and induced apoptosis significantly through mitochondria-related pathways. Human apoptosis protein array assay also demonstrated 15a increased the expression levels of pro-apoptotic Bax, Bad, HtrA2 and Trail R2/DR5. The expression of catalase and cell cycle blocker claspin were similarly up-regulated. In balance, 15a induced K562 cells death through both endogenous and exogenous pathways.

Identification of New Nitric Oxide-Donating Peptides with Dual Biofilm Eradication and Antibacterial Activities for Intervention of Device-Related Infections

Implantable medical device-related infections with biofilms have become a significant challenge in clinics. Based on the potential bacteria biofilm dispersing effect of nitric oxide (NO) and the unique antibacterial activity of antimicrobial peptides (AMP), we synthesized five peptides and selected the most potent one to conjugate its N-terminal with a furoxan moiety to offer a hitherto unknown NO-donating antimicrobial peptide (FOTyr-AMP), which exhibited Staphylococcus aureus and Escherichia coli biofilm dispersion and eradication, and potent antibacterial activities in vitro. In an implanted biofilm infection mice model, topical subcutaneous injection of FOTyr-AMP allowed synergetic eradication of bacterial biofilms and potent antibacterial activity, superior to the antibiotic cephalosporin C. Given the low hemolysis effect, little influence on the blood pressure, and potent in vivo efficacy of FOTyr-AMP, it is clear that subcutaneous administration of FOTyr-AMP could be a promising approach for the intervention of medical device-related biofilm infections with desirable safety.

NO donor-type large yellow acid derivatives, their preparation method and medical use (by machine translation)

The present invention relates to the field of pharmaceutical chemistry and drug therapeutics, in particular to NO donor-type large yellow acid derivative and its preparation method and application in pharmacy. The compound has anti-tumor effect, can be used for preparing anti-tumor drug. The invention also relates to a method for preparing such compounds. (by machine translation)