Chlorides-buliding-blocks

Shim, Soon-Mi; Bae, Eunkyung; Kim, Gun-Hee published the artcile< Single-dose oral acute toxicity and mutagenic effects of methanol extracts of Cirsium japonicum>, Electric Literature of 6055-19-2, the main research area is Cirsium acute oral toxicity mutagenicity chromosome flavone.

The purpose of this study was to evaluate safety on Cirsium japonicum extracts containing flavones by examining acute oral toxicity, bacterial reverse mutation and the chromosome aberration test. Mutagenicity of extracts were evaluated by a bacterial reverse mutation assay using Salmonella typhimurium TA98, TA100, TA102, TA1535, TA1537 and Escherichia coli (WP2uvrA) with and without metabolic activation. An in vitro chromosome aberration test in Chinese hamster lung cells was conducted at the concentrations of 0, 1,250, 2,500 and 5,000 μg/mL. No significant adverse effects on body weight, mortality and gross findings were observed for 15 days after a single dose (2,000 mg of extracts/kg body weight) of administration. In the bacterial reverse mutation assay, C. japonicum extracts ranging from 156 to 5,000 μg/plate did not induce base-pair substitution or frame shift. Any significant increase in structural aberration as well as reduction of cell cycle progression was not observed in the chromosome.

Journal of Food Biochemistry published new progress about Chromosome aberrations. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Electric Literature of 6055-19-2.

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

Liu, Jinggong; Liu, Weilin; Ge, Hu; Gao, Jinbo; He, Qingqing; Su, Lijuan; Xu, Jun; Gu, Lian-quan; Huang, Zhi-shu; Li, Ding published the artcile< Syntheses and characterization of non-bisphosphonate quinoline derivatives as new FPPS inhibitors>, Computed Properties of 22717-55-1, the main research area is non bisphosphonate quinoline derivative preparation FPPS geranyltransferase inhibitor cancer; 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide; Allosteric site; BPs; BSA; Bisphosphonate; Cancer; DL-dithiothreitol; DTT; FPPS; Farnesyl pyrophosphate synthase; HAP; MTT; Quinoline derivative; Tris; bisphosphonates; bovine serum albumin; farnesyl pyrophosphate synthase; hydroxyapatite; tris(hydroxymethyl)aminomethane.

Background: Farnesyl pyrophosphate synthase (FPPS) is a key regulatory enzyme in the biosynthesis of cholesterol and in the post-translational modification of signaling proteins. It has been reported that non-bisphosphonate FPPS inhibitors targeting its allosteric binding pocket are potentially important for the development of promising anti-cancer drugs. Methods: The following methods were used: organic syntheses of non-bisphosphonate quinoline derivatives, enzyme inhibition studies, fluorescence titration assays, synergistic effect studies of quinoline derivatives with zoledronate, ITC studies for the binding of FPPS with quinoline derivatives, NMR-based HAP binding assays, mol. modeling studies, fluorescence imaging assay and MTT assays. Results: We report our syntheses of a series of quinoline derivatives as new FPPS inhibitors possibly targeting the allosteric site of the enzyme. Compound 6b showed potent inhibition to FPPS without significant hydroxyapatite binding affinity. The compound showed synergistic inhibitory effect with active-site inhibitor zoledronate. ITC experiment confirmed the good binding effect of compound 6b to FPPS, and further indicated the binding ratio of 1:1. Mol. modeling studies showed that 6b could possibly bind to the allosteric binding pocket of the enzyme. The fluorescence microscopy indicated that these compounds could get into cancer cells. Conclusions: Our results showed that quinoline derivative 6b could become a new lead compound for further optimization for cancer treatment. General significance: The traditional FPPS active-site inhibitors bisphosphonates show poor membrane permeability to tumor cells, due to their strong polarity. The development of new non-bisphosphonate FPPS inhibitors with good cell membrane permeability is potentially important.

Biochimica et Biophysica Acta, General Subjects published new progress about Antitumor agents. 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

Qu, Zheng-Wang; Zhu, Hui; Grimme, Stefan published the artcile< Mechanistic Insights for Dimethyl Sulfoxide Catalyzed Aromatic Chlorination Reactions>, Name: 1-Chloropyrrolidine-2,5-dione, the main research area is dimethyl sulfoxide catalyst aromatic chlorination reaction mechanism.

Recently, the DMSO O=SMe2 catalyzed aromatic chlorination reaction using N-chlorosuccinimides (NsCl) under mild conditions has proven useful for bioactive compounds potentially containing various functional groups such as amide and hydroxyl. A novel catalytic mechanism is revealed by extensive DFT calculations using the anisole PhOMe as electron-rich model substrate. The Cl+ transfer from NsCl to O=SMe2 slowly reacts via the S-chloro sulfoxonium O=SClMe2+ to the S-chloro ylide O=SClMeCH2, followed by facile Cl+ transfer from NsCl to the ylide CH2 site to initialize efficient electrophilic Cl+ transfer to nucleophilic substrates. According to the new proposal, the polarizable S and electroneg. O sites of O=SMe2 may act as efficient Cl+ and H+ shuttles, resp., in catalytic aromatic chlorination. If O=SMe2 is present in high concentration, it can trap intermediate SMe2OH+ into a stable H+-bound dimer (SMe2O)2H+ to inhibit efficient protic NsCl activation. These mechanistic insights may be generally useful for the rational design of novel dual functional halonium transfer catalysts.

ChemCatChem published new progress about Activation energy. 128-09-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C4H4ClNO2, Name: 1-Chloropyrrolidine-2,5-dione.

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

Wang, Wentian; Zhang, Lu; Morlock, Lorraine; Williams, Noelle S.; Shay, Jerry W.; De Brabander, Jef K. published the artcile< Design and Synthesis of TASIN Analogues Specifically Targeting Colorectal Cancer Cell Lines with Mutant Adenomatous Polyposis Coli (APC)>, Application of C7H5ClF2O3S, the main research area is preparation TASIN analog targeting colorectal cancer.

Despite advances in targeted anticancer therapies, there are still no small-mol.-based therapies available that specifically target colorectal cancer (CRC) development and progression, the second leading cause of cancer deaths. We previously disclosed the discovery of truncating adenomatous polyposis coli (APC)-selective inhibitor 1 (TASIN-1), a small mol. that specifically targets colorectal cancer cells lines with truncating mutations in the adenomatous polyposis coli (APC) tumor suppressor gene through inhibition of cholesterol biosynthesis. Here, we report a medicinal chem. evaluation of a collection of TASIN analogs and activity against colon cancer cell lines and an isogenic cell line pair reporting on the status of APC-dependent selectivity. A number of potent and selective analogs were identified, including compounds with good metabolic stability and pharmacokinetic properties. The compounds reported herein represent a first-in-class genotype-selective series that specifically target apc mutations present in the majority of CRC patients and serve as a translational platform toward a targeted therapy for colon cancer.

Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 351003-34-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H5ClF2O3S, Application of C7H5ClF2O3S.

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

Rouissi, Kamel; Hamrita, Bechr; Kouidi, Soumaya; Messai, Yosra; Jaouadi, Bassem; Hamden, Khaled; Medimegh, Imen; Ouerhani, Slah; Cherif, Mohamed; Elgaaied, Amel Benammar published the artcile< In vivo prevention of bladder urotoxicity: purified hydroxytyrosol ameliorates urotoxic effects of cyclophosphamide and buthionine sulfoximine in mice>, Formula: C7H17Cl2N2O3P, the main research area is hydroxytyrosol bladder urotoxicity antioxidant cyclophosphamide monohydrate BSO.

Urotoxicity is a troublesome complication associated with cyclophosphamide (CP) and L-buthionine-SR-sulfoximine (BSO) treatment in chemotherapy. With this concern in mind, the present study investigated the potential effects of a hydroxytyrosol extract from olive mill waste (OMW) on urotoxicity induced by acute CP and BSO doses using a Swiss albino mouse model. Toxicity modulation was evaluated by measuring lipid peroxidation (LPO) and antioxidants in urinary bladder. The findings revealed that the hydroxytyrosol extract exerted a protective effect not only on LPO but also on enzymic antioxidants. When compared to the controls, the CP-treated animals underwent significant decreases in the glutathione S-transferase (GST), glutathione reductase (GR), glutathione peroxidase (GP), and catalase (CAT) activities. The level of glutathione (GSH) was also reduced with increased doses of LPO in the CP-treated animals. L-Buthionine-SR-sulfoximine treatment exerted an additive toxic effect on the CP-treated animals. Interestingly, pretreatment with the hydroxytyrosol extract restored the activities of all enzymes back to normal levels and exhibited an overall protective effect on the CP- and BSO-induced toxicities in urinary bladder. The restoration of GSH through the treatment with the hydroxytyrosol extract can play an important role in reversing CP-induced apoptosis and free radical-mediated LPO.

International Journal of Toxicology published new progress about Antioxidants. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Formula: C7H17Cl2N2O3P.

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

Shingdilwar, Shashikant; Dolui, Subrata; Kumar, Devendra; Banerjee, Sanjib published the artcile< Facile access to template-shape-replicated nitrogen-rich mesoporous carbon nanospheres for highly efficient CO2 capture and contaminant removal>, COA of Formula: C9H9Cl, the main research area is nitrogen carbon dioxide capture nanosphere atom transfer radical polymerization.

Rising atm. CO2 levels and water pollution have necessitated new research towards the development of novel CO2 capture materials and innovative methods for wastewater treatment. Herein, we demonstrate a facile fabrication strategy to prepare novel template-shape-replicated nitrogen-rich mesoporous carbon nanospheres (NMCN) with high surface area, pore volume and ordered pore geometry via a combination of in situ co-condensation, surface-confined atom transfer radical polymerization (SC-ATRP) and post-polymerization modification. NMCN exhibited efficient CO2 capture performance and contaminant removal capability from wastewater. This work may open a new direction for the design of novel porous nanomaterials for CO2 capture and other emerging applications.

Materials Advances published new progress about Adsorption (isotherm). 1592-20-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H9Cl, COA of Formula: C9H9Cl.

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

Borges-Gonzalez, Jorge; Garcia-Monzon, Irma; Martin, Tomas published the artcile< Conformational Control of Tetrahydropyran-based Hybrid Dipeptide Catalysts Improves Activity and Stereoselectivity>, Category: chlorides-buliding-blocks, the main research area is aldehyde nitrostyrene dipeptide catalyst enantioselective diastereoselective Michael addition; nitro phenyl alkanal preparation.

It was demonstrated as to how carbohydrates can be used as conformational control units of organocatalysts to tune their catalytic properties was introduced. New hybrid dipeptide-like organocatalysts based on ζ-sugar aminoacids and proline were prepared and tested for the asym. Michael addition of aldehydes to β-nitrostyrenes. Taking full advantage of the modular nature of the carbohydrate motif, both reactivity and stereoselectivity were significantly improved. By simple structural changes, such as the elimination of the methoxy group in the C4 position of the tetrahydropyran ring, we obtained two complementary catalysts that allow accessed to both enantiomers of the γ-nitroaldehydes with excellent yields, diastereoselectivity and enantiomeric excesses between 97 and 99%, using a catalytic load even below 1 mol%.

Advanced Synthesis & Catalysis published new progress about Aldehydes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 5153-70-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClNO2, Category: chlorides-buliding-blocks.

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

Nam, Nguyen-Hai; Huong, Tran Lan; Dung, Do Thi Mai; Dung, Phan Thi Phuong; Oanh, Dao Thi Kim; Park, Sang Ho; Kim, Kyungrok; Han, Byung Woo; Yun, Jieun; Kang, Jong Soon; Kim, Youngsoo; Han, Sang-Bae published the artcile< Synthesis, bioevaluation and docking study of 5-substituted phenyl-1,3,4-thiadiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents>, Application of C8H6ClN3S, the main research area is thiadiazole hydroxamic acid preparation histone deacetylase inhibitor antitumor; 5-phenyl-1,3,4-thiadiazole; cytotoxicity; heterocycle; histone deacetylase (HDAC) inhibitors.

Since the first histone deacetylase (HDAC) inhibitor (Zolinza, widely known as suberoylanilide hydroxamic acid; SAHA) was approved by the Food and Drug Administration for the treatment of T-cell lymphoma in 2006, the search for newer HDAC inhibitors has attracted a great deal of interest of medicinal chemists worldwide. As a continuity of the ongoing research in this area, the authors designed and synthesized a series of thiadiazole-based hydroxamic acids I [R = H, 2-Cl, 4-Me, etc.] as analogs of SAHA and evaluated their biol. activities. A number of compounds in this series, e.g. I [R = H], I [R = 2-Cl], I [R = 4-MeO], were found to possess potent anticancer cytotoxicity and HDAC inhibition effects. These compounds were generally two- to five-fold more potent in terms of cytotoxicity compared to SAHA against five cancer cell lines tested. Docking studies revealed that these hydroxamic acid displayed higher affinities than SAHA toward HDAC8.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Antitumor agents. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Application of C8H6ClN3S.

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

Dub, Pavel A.; Matsunami, Asuka; Kuwata, Shigeki; Kayaki, Yoshihito published the artcile< Cleavage of N-H Bond of Ammonia via Metal-Ligand Cooperation Enables Rational Design of a Conceptually New Noyori-Ikariya Catalyst>, SDS of cas: 67421-02-7, the main research area is ammonia bond cleavage metal ligand cooperation; ionic ruthenium iridium metallacycle Noyori Ikariya precatalyst asym catalysis.

The asym. transfer hydrogenation (ATH) of ketones/imines with Noyori-Ikariya catalyst represents an important reaction in both academia and fine chem. industry. The method allows for the preparation of chiral secondary alcs./amines with very good to excellent optical purities. Remarkably, the same chiral Noyori-Ikariya complex is also a precatalyst for a wide range of other chemo- and stereoselective reductive and oxidative transformations. Among them are enantioselective sulfonamidation of acrylates (intramol. aza-Michael reaction) and carboxylation of indoles with CO2. Development of these catalytic reactions has been inspired by the realized cleavage of the N-H bond of sulfonamides and indoles by the 16e- amido derivative of the 18e- precatalyst via metal-ligand cooperation (MLC). This paper summarizes our efforts to investigate N-H bond cleavage of gaseous ammonia in solution via MLC and reports the serendipitous discovery of a new class of chiral tridentate κ3[N,N’,N”] Ru and Ir metallacycles, derivatives of the famous M-FsDPEN catalysts (M = Ru, Ir). The protonation of these metallacycles by strong acids containing weakly coordinating (chiral) anions generates ionic complexes, which were identified as conceptually novel Noyori-Ikariya precatalysts. For example, the ATH of aromatic ketones with some of these complexes proceeds with up to 99% ee.

Journal of the American Chemical Society published new progress about Aralkyl alcohols Role: SPN (Synthetic Preparation), PREP (Preparation). 67421-02-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C24H36Cl4Ru2, SDS of cas: 67421-02-7.

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