Category: chlorides-buliding-blocks

Nakahara, Takako; Sakaeda, Toshiyuki; Nakamura, Tsutomu; Tamura, Takao; Nishioka, Chiharu; Aoyama, Nobuo; Okamura, Noboru; Shirakawa, Toshiro; Gotoh, Akinobu; Kamigaki, Takashi; Ohno, Masakazu; Kuroda, Yoshikazu; Matsuo, Masafumi; Kasuga, Masato; Okumura, Katsuhiko published the artcile< Chemosensitivity Assessed by Collagen Gel Droplet Embedded Culture Drug Sensitivity Test, and MDR1, MRP1, and MRP2 mRNA Expression in Human Colorectal Adenocarcinomas>, Safety of 2-(Bis(2-chloroethyl)amino)-1,3,2-oxazaphosphinane 2-oxide hydrate, the main research area is chemosensitivity test multidrug resistance antitumor colorectal adenocarcinomas.

Purpose: To evaluate chemosensitivity and its correlation with expression levels of the multidrug resistant transporter (MDR1) and the multidrug resistance-associated proteins 1 and 2 (MRP1, MRP2) mRNA in human colorectal adenocarcinomas. Methods: Colorectal adenocarcinomas were obtained as surgical samples from 25 patients. The chemosensitivity of 12 anticancer drugs was assessed by the collagen gel droplet embedded culture drug sensitivity test (CD-DST). The expression levels of MDR1, MRP1, and MRP2 mRNA in colorectal adenocarcinomas were also evaluated by real-time quant. reverse transcription-polymerase chain reaction (RT-PCR). Results: The chemosensitivity was successfully evaluated for 16 of 25 patients, and the anticancer drugs were effective against the samples showing a relatively high growth rate. Gemcitabine hydrochloride was found to be more promising than those often prescribed for the treatment of colorectal adenocarcinoma. There was no correlation of the mRNA expression levels of MDR1 and MRP1 with the chemosensitivity of any anticancer drugs tested, but mitomycin C was found to be more effective for the colorectal adenocarcinoma with relatively high expression of MRP2 mRNA.

Pharmaceutical Research published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (MRP1). 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Safety of 2-(Bis(2-chloroethyl)amino)-1,3,2-oxazaphosphinane 2-oxide hydrate.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Atli Sekeroglu, Zulal; Gediz Erturk, Aliye; Kontas Yedier, Seval; Sekeroglu, Vedat published the artcile< In vitro cytogenetic activity of 3-amino-4-[4-(dimethylamino)phenyl]-4,5-dihydro-1,2,5-thiadiazole 1,1-dioxide>, Reference of 6055-19-2, the main research area is amino dimethylamino phenyl dihydro thiadiazole dioxide cytogenetic activity; 1,2,5-Thiadiazole 1,1-dioxide; chromosome aberrations; cytotoxicity; lymphocytes; micronucleus.

In a previous study, 3-amino-4-[4-(dimethylamino)phenyl]-4,5-dihydro-1,2,5-thiadiazole 1,1-dioxide (DPTD), which is five-membered cyclosulfamide, was synthesized and structurally characterized. The aim of this study was to investigate the cytotoxic and genotoxic effects of DPTD on cultured human lymphocytes in the presence and absence of a metabolic activation system (S9 mix). The cytotoxicity and genotoxicity of DPTD in human peripheral blood lymphocytes were examined in vitro by using chromosomal aberration (CA) and micronucleus (MN) tests. Mitomycin-C (MMC) for cultures without S9 mix and cyclophosphamide monohydrate (CP) for cultures with S9 mix were used as pos. controls. The cultures were treated with DPTD (45, 90, and 180μg/mL) in the absence and presence of S9 mix. The cells were also co-treated with DPTD together with MMC or CP. DPTD showed cytotoxic activity due to decreases in mitotic index (MI) and nuclear division index (NDI) in the absence and presence of S9 mix. DPTD also increased the CAs, aberrant cells with CAs and MN values in cultures with and without S9 mix. When DPTD and MMC or CP were used together, lower MI and NDI values and higher CA and MN values were found than those DPTD treated alone. Both DPTD and its metabolites have cytotoxic, cytostatic and genotoxic potential on human peripheral blood lymphocyte cultures under the exptl. conditions. Furthermore, co-treatment of DPTD and MMC or CP can cause more cytotoxicity and genotoxicity. Our results indicated that the use of DPTD with other chemotherapeutic drugs may display more effective results.

Drug and Chemical Toxicology (1977) published new progress about Genotoxicity. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Reference of 6055-19-2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Li, Yuanheng; Sun, Lilan; Yang, Taoyi; Jiao, Wenxuan; Tang, Jingshu; Huang, Xiaomin; Huang, Zongze; Meng, Ying; Luo, Laichun; Wang, Xintong; Bian, Xiling; Zhang, Fang; Wang, KeWei; Sun, Qi published the artcile< Design and Synthesis of Novel Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice>, Application of C7H8ClN, the main research area is thiazolo pyrimidinone preparation nicotinic acetylcholine receptor allosteric modulator SAR.

A series of novel thiazolo[4,5-d]pyrimidin-7(6H)-ones were designed, synthesized, and evaluated as the type I pos. allosteric modulators of human α7 nAChR expressed in Xenopus oocytes by a two-electrode voltage clamp. The structure-activity relationship anal. identified the compound I as a potent and efficacious PAM with the maximum activation effect of the α7 current of over 1633% in the presence of acetylcholine (100 μM) and an EC50 = 1.26 μM. It is highly specific to α7 nAChR over other subtypes of nAChR, 5-HT3A, NMDA, and GABAA receptors. Compound I showed an elimination half-life of 10.8 ± 1.5 h for 3 mg/kg, i.v., and 7.4 ± 1.1 h for 60 mg/kg, i.g. in rat. It also exhibited sufficient blood-brain barrier penetration with no significant effect on hERG channel. Most importantly, compound I dose-dependently (0.1-1 mg/kg, i.p.) reversed the prepulse inhibition deficit induced by MK-801 in the mouse schizophrenia model.

Journal of Medicinal Chemistry published new progress about 5-HT3A receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 29027-20-1 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H8ClN, Application of C7H8ClN.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Yan, Jingling; Wang, Zhen; Gao, Lianxun; Ding, Mengxian published the artcile< Synthesis and properties of polyimides from isomeric bis(dicarboxylphenylthio)diphenyl sulfone dianhydrides>, Recommanded Product: 5-Chloroisobenzofuran-1,3-dione, the main research area is isomeric tetracarboxylic dianhydride polyimide polysulfone preparation property; permeability permselectivity oxygen nitrogen polyimide polysulfone.

4,4′-Bis(3,4-dicarboxyphenylthio)diphenyl sulfone dianhydride(4,4′-PTPSDA) and 4,4′-bis(2,3-dicarboxyphenylthio)diphenyl sulfone dianhydride(3,3′-PTPSDA) were synthesized from chlorophthalic anhydrides and bis(4-mercaptophenyl)sulfone. Their structures were determined via IR spectra, 1H NMR and elemental anal. A series of polyimides were prepared from isomeric PTPSDAs and aromatic diamines in 1-methyl-2-pyrrolidinone (NMP) via the conventional two-step method. Polyimides based on 4,4′-PTPSDA and 3,3′-PTPSDA have good solubility in polar aprotic solvents and phenols. The 5% weight-loss temperatures of isomeric polyimides were near 500 °C in N2. DMTA and DSC analyses indicated that the glass-transition temperatures of polyimides from 3,3′-PTPSDA are higher than those of polyimides from 4,4′-PTPSDA. The wide-angle X-ray diffraction showed that all polyimides are amorphous. The polyimides from 3,3′-PTPSDA showed higher permeability but lower permselectivity compared with those from 4,4′-PTPSDA.

Polymer published new progress about Elongation at break. 118-45-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H3ClO3, Recommanded Product: 5-Chloroisobenzofuran-1,3-dione.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Hu, Xiaojun; Zhou, Bingwei; Jin, Hongwei; Liu, Yunkui; Zhang, Liming published the artcile< Bifunctional phosphine ligand-enabled gold-catalyzed direct cycloisomerization of alkynyl ketones to 2,5-disubstituted furans>, COA of Formula: C9H7ClO, the main research area is disubstituted furan preparation phosphinyl gold catalyst; alkynyl ketone cycloisomerization.

An efficient synthesis of 2,5-disubstituted furans I (R1 = H, 4-Me, 4-F, etc.; R2 = Pr, C6H5, Bn, etc.) directly from alkynyl ketones has been developed via tandem gold(I)-catalyzed isomerization of alkynyl ketones to allenyl ketones and cycloisomerization. The key to the success of this chem. is the use of a biphenyl-2-ylphosphine ligand featuring a critical remote tertiary amino group.

Chemical Communications (Cambridge, United Kingdom) published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 17082-09-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H7ClO, COA of Formula: C9H7ClO.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Carrillo-Arcos, Ulises A.; Rojas-Ocampo, Jonathan; Porcel, Susana published the artcile< Oxidative cyclization of alkenoic acids promoted by AgOAc>, Computed Properties of 22717-55-1, the main research area is benzodioxinone preparation; oxidative cyclization alkenoic acid silver acetate.

Alkenoic acids derived from salicylic acid and analogs undergo an unexpected oxidative cyclization process triggered by AgOAc leading to 4H-benzo[d][1,3]dioxin-4-ones. The process is affected by the substitution on the aryl and the allyl units.

Dalton Transactions published new progress about Carboxylic acids, unsaturated Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 22717-55-1 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO3, Computed Properties of 22717-55-1.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Ji, Shunli; Gao, Hongbin; Xia, Xingya; Zheng, Feng published the artcile< A new HPLC-UV derivatization approach for the determination of potential genotoxic benzyl halides in drug substances>, Related Products of 611-19-8, the main research area is benzyl halide antipyrine oroxylin A genotoxicity HPLCUV derivatization method.

Benzyl halides, widely used as alkylation reagents in drug synthesis, are potential genotoxic impurities (PGTIs) required to be controlled at trace levels. However, the existing anal. methods for benzyl halides often suffer from matrix interferences or low derivatization efficiency of benzyl chlorides. In this paper, a simple derivatization HPLC-UV method was developed for the anal. of these residual trace benzyl halides in drug substances. 1-(4-Nitrophenyl) piperazine (4-NPP) was selected as a new derivatization reagent because it shifted well the benzyl halides derivatives away to the near visible range (392 nm), which could minimize the matrix interferences from the drug substances and related impurities. Meanwhile, potassium iodide (KI) was used to convert the mixed benzyl halides into benzyl iodides before derivatization. The derivatization parameters were also optimized using the design of experiments (DoE) for achieving the best reaction efficiency. The results showed that the new approach had high specificity and sensitivity, and the LOQs were 7-9 μg g-1 relative to 5 mg mL-1 antipyrine and 17.5-22.5 μg g-1 relative to 2 mg mL-1 oroxylin A. The method is a valuable alternative for the determination of residual benzyl halides in the drug substances.

RSC Advances published new progress about Benzyl halides Role: ANT (Analyte), ANST (Analytical Study). 611-19-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2, Related Products of 611-19-8.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Dukat, Ma-lgorzata; Abdel-Rahman, Ashraf A.; Ismaiel, Abd M.; Ingher, Stacy; Teitler, Milt; Gyermek, Lazlo; Glennon, Richard A. published the artcile< Structure-Activity Relationships for the Binding of Arylpiperazines and Arylbiguanides at 5-HT3 Serotonin Receptors>, Quality Control of 16799-05-6, the main research area is arylpiperazine arylbiguanide preparation serotonin receptor binding.

Arylpiperazines are nonselective agents that bind at 5-HT3 serotonin receptors with moderate to high affinity, whereas 1-phenylbiguanide is a low-affinity but more selective 5-HT3 agonist. In an attempt to enhance the affinity of the latter agent, and working with the assumption that similarities might exist between the binding of the two types of agents, we formulated structure-activity relationships for the binding of the arylpiperazines and then incorporated those substituents, leading to high affinity for the arylpiperazines, into 1-phenylbiguanide. A subsequent investigation examined the structure-activity relationships of the arylbiguanides and identified arylguanidines as a novel class of 5-HT3 ligands. Although curious similarities exist between the structure-activity relationships of the arylpiperazines, arylbiguanides, and arylguanidines, it cannot be concluded that all three series of compounds are binding in the same manner. Furthermore, upon investigating pairs of compounds in the three series, the arylpiperazines behaved as 5-HT3 antagonists (von Bezold-Jarisch assay) whereas the arylbiguanides and arylguanidines acted as 5-HT3 agonists.

Journal of Medicinal Chemistry published new progress about 5-HT3 receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Quality Control of 16799-05-6.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Gao, Changlu; Zhang, Suobo; Gao, Lianxun; Ding, Mengxian published the artcile< Microwave-assisted synthesis of high-molecular-weight poly(ether imide)s by phase-transfer catalysis>, Synthetic Route of 118-45-6, the main research area is polyether polyimide polycondensation phase transfer catalysis polymerization microwave.

A facile and rapid polycondensation reaction of disodium bisphenol A with bis(chlorophthalimide)s was preformed with a domestic microwave oven in o-dichlorobenzene by phase-transfer catalysis. The polymerization reactions, in comparison with conventional heating polycondensation, proceeded rapidly and were completed within 25 min. The polymerizations gave the corresponding poly(ether imide)s with inherent viscosities of 0.55-0.92 dL g-1. The effects of various factors on the polymerization, such as the amount of the catalyst, the reaction time, and the microwave power were studied. The properties of the polymers were briefly characterized.

Journal of Applied Polymer Science published new progress about Glass transition temperature. 118-45-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H3ClO3, Synthetic Route of 118-45-6.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Yamaguchi, Miyuki; Katsumata, Haruka; Manabe, Kei published the artcile< One-Pot Synthesis of Substituted Benzo[b]furans from Mono- and Dichlorophenols Using Palladium Catalysts Bearing Dihydroxyterphenylphosphine>, Application of C8H7ClO3, the main research area is Sonogashira Suzuki Miyaura coupling chlorophenol alkyne boronic acid; palladium dihydroxyterphenylphosphine XPhos catalyst benzofuran preparation.

A dihydroxyterphenylphosphine bearing cyclohexyl groups on the phosphorus atom (I, Cy-DHTP) was found to be a powerful ligand for the palladium-catalyzed one-pot synthesis of substituted benzo[b]furans from 2-chlorophenols and terminal alkynes. E.g., in presence of PdCl2(MeCN)2, I, and LiOCMe3, Sonogashira cross-coupling of 2-chlorophenol and PhCH2CH2CCH gave 82% benzo[b]furan derivative (II). This catalyst system was also applicable to the sequential one-pot synthesis of disubstituted benzo[b]furans from dichlorophenols via the Suzuki-Miyaura cross-coupling of chlorobenzo[b]furan with boronic acids. The use of two ligands, I and XPhos, is the key to promoting the reactions. Mechanistic studies suggest that the Pd-Cy-DHTP catalyst is the active species in the Sonogashira cross-coupling step, while the Pd-XPhos catalyst accelerates the Suzuki-Miyaura cross-coupling step.

Journal of Organic Chemistry published new progress about Alkynes, α- Role: RCT (Reactant), RACT (Reactant or Reagent). 3964-57-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO3, Application of C8H7ClO3.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics