619-67-0Relevant articles and documents
Selective detection of cyanide ion in 100 % water by indolium based dual reactive binding site optical sensor
Jayasudha, Palanisamy,Manivannan, Ramalingam,Park, Jong Ho,Son, Young-A
, (2020)
The indolium based sensor (R) system was designed, synthesized, characterized and its cyanide recognizing abilities are examined in 100 % water. The sensor attach with cyanide ion through nucleophilic addition to C atom of the indolium C[dbnd]N group. Also the sensor displayed colorimetric and fluorimetric behavior and it can be simply observed by naked eye. The addition of other chosen anions does not affect the sensor response towards cyanide ion. Test strip constructed on R was act as a convenient test kit to distinguish cyanide ion. Besides, the recognizing ability of sensor has been effectively applied in real water samples and this was validated with HPLC technique. Thus the receptor can be used as an effective sensor to sense cyanide ion water.
Exploiting the 4-hydrazinobenzoic acid moiety for the development of anticancer agents: Synthesis and biological profile
Abuelizz, Hatem A.,Awad, Hanem M.,Marzouk, Mohamed,Nasr, Fahd A.,Bakheit, Ahmed H.,Naglah, Ahmed M.,Al-shakliah, Nasser S.,Al-Salahi, Rashad
, (2020)
Thirteen 4-hydrazinobenzoic acid derivatives were elaborated and characterized by spectral analyses (NMR and MS). Evaluation of their in vitro cytotoxic activity showed that some of the targets demonstrated potent inhibitory effects against HCT-116 and MC
Novel benzenesulfonamides aryl and arylsulfone conjugates adopting tail/dual tail approaches: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies
Eldeeb, Assem H.,Abo-Ashour, Mahmoud F.,Angeli, Andrea,Bonardi, Alessandro,Lasheen, Deena S.,Elrazaz, Eman Z.,Nocentini, Alessio,Gratteri, Paola,Abdel-Aziz, Hatem A.,Supuran, Claudiu T.
supporting information, (2021/05/10)
New series of benzenesulfonamide and benzoic acid derivatives were designed and synthesized using tail/dual tail approach to improve potency and selectivity as carbonic anhydrase inhibitors. The synthesized compounds evaluated as CAIs against isoforms hCA I, II, IV and IX with acetazolamide (AAZ) as standard inhibitor. The benzenesulfonamide derivatives 7a-d, 8a-h, 12a-c, 13a and 15a-c showed moderate to potent inhibitory activity with selectivity toward isoform hCA II, especially, compound 13a with (Ki = 7.6 nM), while the benzoic acid analogues 12d-f, 13b and 15d-f didn't show any activity except compounds 12d,f and 15e that showed weak activity. Additionally, molecular docking was performed for compounds 7a, 8a, 8e, 12a, 13a and 15a on isoform hCA I, II to illustrate the possible interaction with the active site to justify the inhibitory activity.
Discovery of novel inhibitors of human phosphoglycerate dehydrogenase by activity-directed combinatorial chemical synthesis strategy
Gou, Kun,Luo, Youfu,Luo, Yuan,Sun, Qingxiang,Tan, Yuping,Tao, Lei,Zhao, Yinglan,Zhou, Xia,Zhou, Yue,Zuo, Zeping
, (2021/07/26)
Serine, the source of the one-carbon units essential for de novo purine and deoxythymidine synthesis plays a crucial role in the growth of cancer cells. Phosphoglycerate dehydrogenase (PHGDH) which catalyzes the first, rate-limiting step in de novo serine biosynthesis has become a promising target for the cancer treatment. Here we identified H-G6 as a potential PHGDH inhibitor from the screening of an in-house small molecule library based on the enzymatic assay. We adopted activity-directed combinatorial chemical synthesis strategy to optimize this hit compound. Compound b36 was found to be the noncompetitive and the most promising one with IC50 values of 5.96 ± 0.61 μM against PHGDH. Compound b36 inhibited the proliferation of human breast cancer and ovarian cancer cells, reduced intracellular serine synthesis, damaged DNA synthesis, and induced cell cycle arrest. Collectively, our results suggest that b36 is a novel PHGDH inhibitor, which could be a promising modulator to reprogram the serine synthesis pathway and might be a potential anticancer lead worth further exploration.
Spontaneous optical response towards cyanide ion in water by a reactive binding site probe
Jayasudha, Palanisamy,Manivannan, Ramalingam,Park, Jong Ho,Son, Young-A
supporting information, (2020/03/10)
Indolium derivatives bearing diphenyl amine (R1) and dibenzylamine (R2) linked through benzene was designed, synthesized, characterized and its cyanide recognizing abilities are studied in 100% water. The probes were exhibited dual channel properties i.e. both colorimetric and fluorimetric changes for the effective sensing of cyanide ion. The discrete color variation of probes with cyanide ion makes possible as colorimetric sensor and which was seen easily through naked eye. The recognition of cyanide ion is accomplished via the attachment of cyanide ion at the C atom of indolium C[dbnd]N group through nucleophilic addition. Also, the found detection limits of probes (nM range) were much lower than the WHO limit. Besides, the probes were effectively applied to determine cyanide ion in real water samples and thus was confirmed with HPLC method.
METHOD FOR MANUFACTURING HYDRAZINO ARYL CARBOXYLIC ACID
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Paragraph 0029, (2016/11/17)
PROBLEM TO BE SOLVED: To provide a method simple and advantageous even in performance on an industrial scale in production of hydrazino aryl carboxylic acids useful as a functional intermediate in pharmaceutical and agrochemical fields, or the like. SOLUTION: The method for manufacturing hydrazino aryl carboxylic acids comprises: smoothly proceeding a reaction by reacting carboxy aryl halides or carboxy aryl sulfones with hydrazines in the presence of water using copper, copper salts and/or palladium, palladium salts and bases; and obtaining hydrazino aryl carboxylic acids by simply separating crystals by acid precipitation operation, and can be performed on an industrial scale. COPYRIGHT: (C)2015,JPOandINPIT
Synthesis and antifungal activity of substituted 2,4,6-pyrimidinetrione carbaldehyde hydrazones
Neumann, Donna M.,Cammarata, Amy,Backes, Gregory,Palmer, Glen E.,Jursic, Branko S.
, p. 813 - 826 (2014/01/23)
Opportunistic fungal infections caused by the Candida spp. are the most common human fungal infections, often resulting in severe systemic infections - a significant cause of morbidity and mortality in at-risk populations. Azole antifungals remain the mainstay of antifungal treatment for candidiasis, however development of clinical resistance to azoles by Candida spp. limits the drugs' efficacy and highlights the need for discovery of novel therapeutics. Recently, it has been reported that simple hydrazone derivatives have the capability to potentiate antifungal activities in vitro. Similarly, pyrimidinetrione analogs have long been explored by medicinal chemists as potential therapeutics, with more recent focus being on the potential for pyrimidinetrione antimicrobial activity. In this work, we present the synthesis of a class of novel hydrazone-pyrimidinetrione analogs using novel synthetic procedures. In addition, structure-activity relationship studies focusing on fungal growth inhibition were also performed against two clinically significant fungal pathogens. A number of derivatives, including phenylhydrazones of 5-acylpyrimidinetrione exhibited potent growth inhibition at or below 10 μM with minimal mammalian cell toxicity. In addition, in vitro studies aimed at defining the mechanism of action of the most active analogs provide preliminary evidence that these compound decrease energy production and fungal cell respiration, making this class of analogs promising novel therapies, as they target pathways not targeted by currently available antifungals.
Methods and Compositions for Modulating P300/CBP Activity
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Page/Page column 19, (2010/09/05)
The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain.
Virtual ligand screening of the p300/CBP histone acetyltransferase: Identification of a selective small molecule inhibitor
Bowers, Erin M.,Yan, Gai,Mukherjee, Chandrani,Orry, Andrew,Wang, Ling,Holbert, Marc A.,Crump, Nicholas T.,Hazzalin, Catherine A.,Liszczak, Glen,Yuan, Hua,Larocca, Cecilia,Saldanha, S. Adrian,Abagyan, Ruben,Sun, Yan,Meyers, David J.,Marmorstein, Ronen,Mahadevan, Louis C.,Alani, Rhoda M.,Cole, Philip A.
scheme or table, p. 471 - 482 (2011/08/06)
The histone acetyltransferase (HAT) p300/CBP is a transcriptional coactivator implicated in many gene regulatory pathways and protein acetylation events. Although p300 inhibitors have been reported, a potent, selective, and readily available active-sitedirected small molecule inhibitor is not yet known. Here we use a structure-based, in silico screening approach to identify a commercially available pyrazolone- containing small molecule p300 HAT inhibitor, C646. C646 is a competitive p300 inhibitor with a Ki of 400 nM and is selective versus other acetyltransferases. Studies on site-directed p300 HAT mutants and synthetic modifications of C646 confirm the importance of predicted interactions in conferring potency. Inhibition of histone acetylation and cell growth by C646 in cells validate its utility as a pharmacologic probe and suggest that p300/CBP HAT is a worthy anticancer target.
Advanced glycation inhibitors containing amino-benzoic acids and derivatives, and methods of use
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, (2008/06/13)
The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylaton endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
