Author: Jessica.F

Yadav, Mange R.; Grande, Fedora; Chouhan, Bishram S.; Naik, Prashant P.; Giridhar, Rajani; Garofalo, Antonio; Neamati, Nouri published the artcile< Cytotoxic potential of novel 6,7-dimethoxyquinazolines>, Related Products of 5004-88-6, the main research area is dimethoxyquinazoline preparation; cancer anticancer cytotoxicity human structure activity.

The synthesis and cytotoxicity of a series of substituted 6,7-dimethoxyquinazoline derivatives, e.g., I, is reported. The cytotoxic activity of all synthesized compounds has been evaluated against HCT116p53+/+ and HCT116p53-/- colon cancer cells and a HEY ovarian cancer cell line naturally resistant to cisplatin. Nine of the tested compounds showed significant cytotoxicity in all cell lines at 10 μM. The most promising derivative I showed IC50values of 0.7 and 1.7 μM in the two colon cancer cell lines.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Related Products of 5004-88-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Alhamd, Mehdi; Tabatabaie, Tayebeh; Parseh, Iman; Amiri, Fazel; Mengelizadeh, Nezamaddin published the artcile< Magnetic CuNiFe2O4 nanoparticles loaded on multi-walled carbon nanotubes as a novel catalyst for peroxymonosulfate activation and degradation of reactive black 5>, COA of Formula: C6H6ClNO2S, the main research area is copper nickel ferrite carbon nanotube reactive black catalytic degradation; By-products; Degradation pathways; MWCNTs-CuNiFe2O4; Peroxymonosulfate; Real wastewater.

Novel copper-nickel ferrite nanocatalyst loaded on multi-walled carbon nanotube (MWCNTs-CuNiFe2O4) was synthesized and applied to activate peroxymonosulfate (PMS) in the degradation of the reactive black 5 (RB5). The structure of the catalyst was well characterized by scanning electron microscope (SEM), Fourier-transform IR spectroscopy (FTIR), and X-ray powder diffraction (XRD). The MWCNTs-CuNiFe2O4/PMS system showed a high performance in the degradation of RB5 with a kinetic rate of 1.5-2.5 times higher than homogeneous and heterogeneous systems. Maximum degradation efficiency (99.60%) was obtained at an initial pH of 7, catalyst dosage of 250 mg/L, PMS dosage of 4 mM, the temperature of 25°C, and reaction time of 15 min. Anion experiments emphasized that the presence of nitrate, carbonate, and phosphate in the solution reduced the degradation efficiency by producing reactive species with low oxidation potential. The RB5 degradation rate evolved with temperature, and the activation energy was obtained to be 44.48 kJ/mol. The mechanism of PMS activation and production of free radicals was proposed based on tert-Bu alc. (TBA), ethanol (EtOH), and potassium iodide (KI) scavengers. Trapping experiments showed that both sulfate (SO4·-) and hydroxyl (·OH) radicals are involved in the catalytic degradation of RB5. The effective treatment of real wastewater and tap water by the MWCNTs-CuNiFe2O4/PMS system requires a long reaction time. Gas chromatog.-mass spectrometry (GC-MS) anal. indicated that RB5 can be degraded via methylation, decarboxylation, hydroxylation, and ring/chain cleavage pathways. The stable catalytic activity after three consecutive cycles suggested that MWCNTs-CuFe2O4 is a novel reusability catalyst in PMS activation. Graphical abstract: [graphic not available: see fulltext].

Environmental Science and Pollution Research published new progress about Activation energy. 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, COA of Formula: C6H6ClNO2S.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Kannan, Shanmugaperumal; Chetty, Kuna Venugopal; Venugopal, Venkatarama; Drew, Michael G. B. published the artcile< Extraction and coordination studies of the unexplored bifunctional ligand carbamoyl methyl sulfoxide (CMSO) with uranium(VI) and cerium(III) nitrates. Synthesis and structures of [UO2(NO3)2(PhSOCH2CONiBu2)] and [Ce(NO3)3(PhSOCH2CONBu2)2]>, Electric Literature of 5326-82-9, the main research area is carbamoylmethylsulfoxide preparation complexation cerium uranyl; cerium carbamoylmethylsulfoxide complex preparation; uranyl carbamoylmethylsulfoxide complex preparation; crystal structure cerium uranyl carbamoylmethylsulfoxide complex; extraction actinide carbamoylmethylsulfoxide.

The bifunctional carbamoyl Me sulfoxide ligands, PhCH2SOCH2CONHPh (L1), PhCH2SOCH2CONHCH2Ph (L2), PhSOCH2CONiPr2 (L3), PhSOCH2CONBu2 (L4), PhSOCH2CONiBu2 (L5) and PhSOCH2CON(C8H17)2 (L6) were synthesized and characterized by spectroscopic methods. The selected coordination chem. of L1, L3, L4 and L5 with [UO2(NO3)2] and [Ce(NO3)3] was evaluated. The structures of [UO2(NO3)2(PhSOCH2CONiBu2)] (10) and [Ce(NO3)3(PhSOCH2CONBu2)2] (12) were determined by single crystal x-ray diffraction methods. Preliminary extraction studies of ligand L6 with U(VI), Pu(IV) and Am(III) in tracer level showed an appreciable extraction for U(VI) and Pu(IV) in up to 10 M HNO3 but not for Am(III). Thermal studies on compounds [UO2(NO3)2( PhSOCH2CONiPr2)] (8) and 10 in air revealed that the ligands can be destroyed completely on incineration. The electron spray mass spectra of compounds 8 and 10 in acetone show that extensive ligand distribution reactions occur in solution to give a mixture of products with ligand to metal ratios of 1:1 and 2:1. However, 10 retains its solid state structure in CH2Cl2.

Dalton Transactions published new progress about Actinides Role: PEP (Physical, Engineering or Chemical Process), PROC (Process). 5326-82-9 belongs to class amides-buliding-blocks, and the molecular formula is C10H20ClNO, Electric Literature of 5326-82-9.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Dully, Michele; Brasnett, Christopher; Djeghader, Ahmed; Seddon, Annela; Neilan, John; Murray, David; Butler, James; Soulimane, Tewfik; Hudson, Sarah P. published the artcile< Modulating the release of pharmaceuticals from lipid cubic phases using a lipase inhibitor>, Related Products of 96829-58-2, the main research area is pharmaceutical lipid cubic system controlled release monoglyceride lipase inhibitor; Controlled delivery; Enzyme degradation; Hydrophobic active pharmaceuticals; Lipase inhibitor; Lipid cubic phase; SAXS.

Lipid cubic phase formulations have gained recognition as potential controlled delivery systems for a range of active pharmaceutical and biol. agents on account of their desirable physiochem. properties and ability to encapsulate both hydrophobic and hydrophilic mols. The most widely studied lipid cubic systems are those of the monoacylglycerol lipid family. These formulations are susceptible to lipolysis by a variety of enzymes, including lipases and esterases, which attack the ester bond present on the lipid chain bridging the oleic acid component to the glycerol backbone. The release of poorly soluble mols. residing in the lipid membrane portions of the phase is limited by the breakdown of the matrix; thus, presenting a potential means for further controlling and sustaining the release of therapeutic agents by targeting the matrix stability and its rate of degradation The aims of the present study were twofold: to evaluate an approach to regulate the rate of degradation of lipid cubic phase drug delivery systems by targeting the enzyme interactions responsible for their demise; and to study the subsequent drug release profiles from bulk lipid cubic gels using model drugs of contrasting hydrophobicity. Here, hybrid materials consisting of cubic phases with monoacylglycerol lipids of different chain lengths formulated with a potent lipase inhibitor tetrahydrolipstatin were designed. Modulation of the release of a hydrophobic model pharmaceutical, a clofazimine salt, was obtained by exploiting the matrixes’ enzyme-driven digestion. A stable cubic phase is described, displaying controlled degradation with at least a 4-fold improvement compared to the blank systems shown in inhibitor-containing cubic systems. Sustained release of the model hydrophobic pharmaceutical was studied over 30 days to highlight the advantage of incorporating an inhibitor into the cubic network to achieve tunable lipid release systems. This is done without neg. affecting the structure of the matrix itself, as shown by comprehensive small-angle x-ray scattering experiments

Journal of Colloid and Interface Science published new progress about Biodegradation kinetics. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Related Products of 96829-58-2.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Zhang, Zhanwen; Liu, Shaoyu; Ma, Hui; Nie, Dahong; Wen, Fuhua; Zhao, Jing; Sun, Aixia; Yuan, Gongjun; Su, Shu; Xiang, Xianhong; Hu, Ping; Tang, Ganghua published the artcile< Validation of R-2-[18F]Fluoropropionic Acid as a Potential Tracer for PET Imaging of Liver Cancer>, Application In Synthesis of 96829-58-2, the main research area is liver cancer radioactivity tracer PET imaging; 2-[18F]Fluoropropionic acid; Liver cancer; Positron emission tomography; R,S-enantiomer; Uptake mechanism.

2-[18F]Fluoropropionic acid (RS-[18F]FPA) has shown potential value as a short-chain fatty acid positron emission tomog. (PET) tracer for the detection of liver cancer. However, RS-[18F]FPA is a mixture of 2-R-[18F]fluoropropionic acid (R-[18F]FPA) and 2-S-[18F]fluoropropionic acid (S-[18F]FPA). The aim of this study is to validate the feasibility of R-[18F]FPA in preclin. PET imaging of liver cancer and to compare the use of R-[18F]FPA with that of RS-[18F]FPA and S-[18F]FPA. A comparative study of R-[18F]FPA, RS-[18F]FPA, S-[18F]FPA, and [18F]FDG micro-PET imaging was performed in HepG2 and SK-Hep-1 tumor-bearing mice. A comparison of R-[18F]FPA uptake with that of S-[18F]FPA by HepG2 and SK-Hep-1 cells was made at different time points. Addnl., in vivo blocking experiments in HepG2 and SK-Hep-1 tumor models were conducted with orlistat and 3-nitropropionic acid (3-NP). In vitro blocking experiments with orlistat or 3-NP were performed with HepG2 and SK-Hep-1 cells. The radioactivity uptake values of R-[18F]FPA were comparable to those of RS-[18F]FPA but were higher than those of S-[18F]FPA and 2-deoxy-2-[18F]fluoro-D-glucose ([18F]FDG) in HepG2 tumors. The radioactivity uptake values of R-[18F]FPA in large HepG2 tumors were lower than those of [18F]FDG (P < 0.05), while R-[18F]FPA PET was significantly superior to [18F]FDG PET in detecting small tumors (both SK-Hep-1 and HepG2 tumors). The in vivo PET imaging experiments showed that R-[18F]FPA uptake in HepG2 tumor-bearing mice was blocked by 19.3 % and 31.8 % after treatment with orlistat and 3-NP, resp. The radioactivity uptake values of R-[18F]FPA in SK-Hep-1 tumor-bearing mice was blocked by 39.5 % with orlistat. R-[18F]FPA seems to be more potential than S-[18F]FPA as an optically pure PET probe, with effective compensation for the deficiencies of [18F]FDG, particularly in PET imaging of small liver cancer. The uptake mechanism of [18F]FPA in liver cancer may be related to fatty acid synthesis and the tricarboxylic acid cycle. However, compared with the racemic RS-[18F]FPA, the possible advantages of R-enantiomer R-[18F]FPA still needs further research. Molecular Imaging and Biology published new progress about Adenocarcinoma. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Application In Synthesis of 96829-58-2.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Cui, Xinyuan; Chen, Xiaojun; Li, Yifu; Fu, Xiao; Song, Pan’ai; Xiao, Li; Sun, Lin; Liu, Hong; Zhu, Xuejing; Yuan, Shuguang published the artcile< Oxalate crystal-related acute renal injury caused by orlistat: A case report.>, Category: amides-buliding-blocks, the main research area is acute oxalic acid nephropathy; hyperoxaluria; orlistat.

We reported a case of oxalate crystal-related acute kidney injury caused by orlistat. The patient was admitted for nephrotic syndrome and acute kidney injury. The pathomorphological assessment of renal biopsy showed intratubular oxalate crystals. The patient reported that she had taken orlistat regularly to loss weight for more than a year. This patient had a habit of drinking vegetable soup and strong herbal tea daily. Orlistat, an intestinal lipase inhibitor, may cause secondary hyperoxaluria, that is, intestinal hyperoxaluria. Dietary habits could be a common precipitating factor for orlistat-relevant hyperoxaluria. It was comprehensively considered to be oxalate crystal-related acute renal injury, and the patient’s renal function recovered gradually after drug withdrawal. Clinicians should pay attention to screening drug-related acute kidney injury including orlistat when observing patients with unexplained acute kidney injury, and renal biopsy should be performed if necessary. It is also important to warn people who take the orlistat for weight loss about the side effects of this drug so as to adjust the eating habits.

Zhong nan da xue xue bao. Yi xue ban = Journal of Central South University. Medical sciences published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Category: amides-buliding-blocks.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Hou, Yunlei; Wu, Shasha; Ma, Longsheng; Bai, Jinying; Liu, Zijian; Zhao, Yanfang published the artcile< Design, synthesis and antitumor activity of novel 6,7-dimethoxyquinazoline derivatives containing diaryl urea moiety>, Product Details of C9H12N2O3, the main research area is sorafenib dimethoxyquinazoline diaryl urea scaffold antitumor lung gastric cancer.

A series of 6,7-dimethoxyquinazoline derivatives connected by diaryl urea scaffolds was designed, synthesized and their in vitro antitumor activities were evaluated. Most of them showed an excellent potency against the four tested cancer cell lines as compared with sorafenib. Particularly, a promising compound 20 was identified, which showed the most potent antitumor activities with IC50 values of 0.08, 0.09, 0.16 and 0.19 μmol/L against H460, HT-29, MKN-45 and MDA-MB-231 cell lines, resp. The structure-activity relationship(SAR) anal. indicated that compounds with dimethylamino or diethylamino group at the C4 position of 6,7-dimethoxyquinazoline moiety exhibited superior activities than compounds bearing morpholino groups.

Chemical Research in Chinese Universities published new progress about Antitumor agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Product Details of C9H12N2O3.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Hou, Hongcen; Zhao, Yongli; Pu, Shouzhi; Chen, Junmin published the artcile< Rhodium-catalyzed direct C-H bond alkynylation of aryl sulfonamides with bromoalkynes>, Application of C6H6ClNO2S, the main research area is alkynyl benzenesulfonamide preparation; aryl sulfonamide bromoalkyne mono alkynylation rhodium catalyst; benzosultam preparation; bromoalkyne aryl sulfonamide alkynylation intramol cyclization cascade rhodium catalyst.

An efficient protocol for the synthesis of ortho-(1-alkynyl)benzenesulfonamides I [R = H, 4-Me, 4-OCF3, etc.] was developed via rhodium-catalyzed direct ortho-mono-alkynylation of aryl sulfonamides with triisopropylsilyl (TIPS)-substituted bromoalkyne. While triethylsilyl or trimethylsilyl (TES or TMS)-substituted bromoalkyne was also amenable to the alkynylation, affording six membered benzosultams II [R1 = TMS, TES; R2 = H, 6-Me, 6-Et, 6-OMe] via the alkynylation/intramol. cyclization cascade reaction. The present protocol displayed high functional group tolerance and broad substrate scope under an air atm. in good to high yields. Mechanistic studies indicated that the reaction proceeded by a turnover limiting C-H activation step and a plausible mechanism was proposed.

Organic & Biomolecular Chemistry published new progress about Alkynes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Application of C6H6ClNO2S.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Joyce, Paul; Dening, Tahnee J.; Meola, Tahlia R.; Gustafsson, Hanna; Kovalainen, Miia; Prestidge, Clive A. published the artcile< Nanostructured clay particles supplement orlistat action in inhibiting lipid digestion: An in vitro evaluation for the treatment of obesity>, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is obesity orlistat antiobesity agent nanostructured clay particle lipid digestion; Anti-obesity; Fat digestion; Lipid digestion; Lipolysis; Obesity; Orlistat.

In this study, nanostructured clay (NSC) particles, fabricated by spray drying delaminated dispersions technologies that regulate energy uptake, to curb the rising trend in obesity statistics. In this study, nanostructured clay (NSC) particles, fabricated by spray drying delaminated dispersions of com. clay platelets (Veegum HS and LAPONITE XLG), were delivered as complimentary, bioactive excipients with the potent lipase inhibitor, orlistat, for the inhibition of fat (lipid) hydrolysis. Simulated intestinal lipolysis studies were performed by observing changes in free fatty acid concentration and revealed that a combinatorial effect existed when NSC particles were co-administered with orlistat, as evidenced by a 1.2- to 1.6-fold greater inhibitory response over 60 min, compared to dosing orlistat alone. Subsequently, it was determined that a multifaceted approach to lipolysis inhibition was presented, whereby NSC particles adsorbed high degrees of lipid (up to 80% of all lipid species present in lipolysis media) and thus phys. shielded the lipid-in-water interface from lipase access, while orlistat covalently attached and blocked the lipase enzyme active site. Thus, the ability for NSC particles to enhance the biopharmaceutical performance and potency of orlistat is hypothesised to translate into promising in vivo pharmacodynamics, where this novel approach is predicted to lead to considerably greater weight reductions for obese patients, compared to dosing orlistat alone.

European Journal of Pharmaceutical Sciences published new progress about Adsorption. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Vyas, Vijyesh K.; Clarkson, Guy J.; Wills, Martin published the artcile< Enantioselective Synthesis of Bicyclopentane-Containing Alcohols via Asymmetric Transfer Hydrogenation>, Quality Control of 1192620-83-9, the main research area is oxomethyl bicyclopentane enantioselective transfer hydrogenation; hydroxymethyl cyclopentane preparation.

Compounds a containing bicyclo[1.1.1]pentane (BCP) adjacent to a chiral center was prepared with high enantiomeric excess through asym. transfer hydrogenation (ATH) of adjacent ketones. In the reduction step, the BCP occupies the position distant from the η6-arene of the catalyst. The reduction was applied to the synthesis of a BCP analog of the antihistamine drug neobenodine.

Organic Letters published new progress about Alcohols Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, Quality Control of 1192620-83-9.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics