Tag: M.W=200-250

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

Richards, Mark L.; Lio, Shirley Cruz; Sinha, Anjana; Banie, Homayon; Thomas, Richard J.; Major, Michael; Tanji, Mark; Sircar, Jagadish C. published the artcile< Substituted 2-phenyl-benzimidazole derivatives: novel compounds that suppress key markers of allergy>, COA of Formula: C8H4ClF3O2, the main research area is phenyl benzimidazole derivative marker allergy.

The pharmacotherapy of allergy and asthma has traditionally focused on the effecter mols. of the allergic cascade, while neglecting targets that play an early role in their development. Reasoning that IgE is central to the expansion of atopic diseases, we identified and extended a novel family of 2-(substituted phenyl)-benzimidazole inhibitors of IgE response. Pharmacol. activity depends on an intact phenylbenzimidazole-bis-amide backbone, and is optimized by the presence of lipophilic terminal groups composed of either bis cycloalkyl or combinations of aliphatic and halogen-substituted aromatic groups. These compounds also inhibit IL-4 and IL-5 responses in T cells and CD23 expression on B cells, with potencies that parallel their inhibition of IgE. The broad profile of these compounds thus underscores their potential for treating the multifarious pathol. of asthma.

European Journal of Medicinal Chemistry published new progress about Allergy. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, COA of Formula: C8H4ClF3O2.

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

Han, Yong; Zheng, Bo; Peng, Yungui published the artcile< Construction of Chiral 2-Substituted Octahydroindoles from Cyclic Ketones and Nitroolefins Bearing only One α-Substituent>, COA of Formula: C8H8BrCl, the main research area is cyclic ketone nitroolefin amine phosphoric acid catalyst Michael addition; gamma nitro ketone preparation enantioselective intramol reductive amination; octahydroindole preparation.

A dual catalytic system was developed following the screening of a series of chiral primary amine catalysts and chiral phosphoric acid catalysts for the Michael addition of cyclic ketones to nitroolefins bearing only one α-substituent. The resulting γ-nitro ketones, which contain a substituent on the carbon connected to the nitro group, were formed in excellent yields (>80%) with high levels of stereoselectivity (up to 94:6 dr and 98% ee) when the reaction was performed in benzene at 0° with 10 mol% of the optimal amine/phosphoric acid combination (1:1) as a catalyst. Subsequent reduction of the nitro group followed by intramol. reductive amination afforded optically active cis-octahydroindole analogs bearing a non-functional substituent at their 2-position.

Advanced Synthesis & Catalysis published new progress about Alkenes, nitro Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, COA of Formula: C8H8BrCl.

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

Shingare, M. S.; Ingle, D. B. published the artcile< Synthesis of 2-(substituted phenyl sulfonamido)-4-(3'-sulfamyl-4'-substituted phenyl)thiazoles - Part II>, Quality Control of 42413-03-6, the main research area is phenylsulfonamidosulfamylphenylthiazole bactericide; sulfamylphenylthiazole phenylsulfonamido bactericide.

Phenylsulfonamidothiazoles I (R = H, Me, Cl, Br; R1 = H, Cl; R2 = H, Me, Cl, NH2) were prepared in 35-52% yields by condensing aminothiazoles II with 3,4-R1R2C6H3SO2Cl. I were devoid of bactericidal activity.

Acta Ciencia Indica, Chemistry published new progress about 42413-03-6. 42413-03-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O2S, Quality Control of 42413-03-6.

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

Thur, Yithachu; Bhalerao, Amit; Munshi, Zaki; Pansare, Nisha; Mann, Klaus; Hanauer, Guido; Kley, Hans-Peter; Nappe, Sandra; Weiss-Haljiti, Cornelia; Ostermann, Claude; Zitt, Christof; Schaefer, Michaela; Mondal, Dibyendu; Ali Siddiki, Afsar; Armugam, Velavan; Gudaghe, Vinod; Gupta, Mahendra; Rayudu, Pramila; Dautzenberg, Frank M.; Das Sarma, Koushik published the artcile< Structure-activity relationships of 2-arylamido-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide derivatives as cannabinoid receptor agonists and their analgesic action>, Category: chlorides-buliding-blocks, the main research area is thienopyrancarboxamide preparation cannabinoid receptor analgesic SAR.

SAR studies were performed on a series of 2-arylamido-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide derivatives as cannabinoid receptor agonists. Starting from a HTS hit both potency and selectivity could be improved. Modifications to the thiophene fusion and C-3 amides were studied. A representative compound 3t (I) produced analgesia when dosed orally in inflammatory pain models of writhing and carrageenan-induced allodynia.

Bioorganic & Medicinal Chemistry Letters published new progress about Allodynia. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Category: chlorides-buliding-blocks.

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

Mutterer, Francis; Weis, Claus D. published the artcile< Halogenated pyridines. V. Fluorinated and brominated pyridine compounds>, COA of Formula: C6H2Cl3NO2, the main research area is fluoropyridine; bromopyridine; chloropyridine fluorination bromination; pyridine chloro fluorination bromination.

Fluoropyridines I (R = F, R1 = Cl, Me, CF3, NO2, R2 = H, R1 = Cl, Me, R2 = Cl) were prepared by treating I (R = Cl, Br) with KF. I (R = Cl, R1 = CF3, R2 = H) was obtained by treating I (R = Cl, R1 =CCl3, R2 = H) with HF or SbF3. The bromopyridines II (R3 = Br; R4 = H, Cl, CH2R3, NO2, CHO, CO2H, CF3, NH2; R5 = H, R3; R6 = H, Cl, NO2) were obtained by brominating II (R3 = Cl) with HBr-HOAc.

Helvetica Chimica Acta published new progress about 54718-39-7. 54718-39-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H2Cl3NO2, COA of Formula: C6H2Cl3NO2.

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

Xu, Pin; Chen, Peng-Yu; Xu, Hai-Chao published the artcile< Scalable Photoelectrochemical Dehydrogenative Cross-Coupling of Heteroarenes with Aliphatic C-H Bonds>, Safety of 2,6-Dichloro-9-methyl-9H-purine, the main research area is heteroarene photoelectrochem dehydrogenative radical cross coupling light; alkylated heteroarene preparation; C−H functionalization; electrochemistry; heterocycles; photoelectrochemistry; radical reactions.

Heteroarenes are structural motifs found in many bioactive compounds and functional materials. Dehydrogenative cross-coupling of heteroarenes with aliphatic C-H bonds provides straightforward access to functionalized heteroarenes from readily available materials. Established methods employ stoichiometric chem. oxidants under conditions of heating or light irradiation By merging electrochem. and photochem., we have achieved efficient photoelectrochem. dehydrogenative cross-coupling of heteroarenes and C(sp3)-H donors through H2 evolution, without the addition of metal catalysts or chem. oxidants. Mechanistically, the C(sp3)-H donor is converted to a nucleophilic carbon radical through H-atom transfer with chlorine atom, which is produced by light irradiation of anodically generated Cl2 from Cl-. The carbon radical then undergoes radical substitution to the heteroarene to afford alkylated heteroarene products.

Angewandte Chemie, International Edition published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Safety of 2,6-Dichloro-9-methyl-9H-purine.

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

Bi, Qing-wei; Shi, Zhi-chuan; Zhao, Zhi-gang; Xia, Zhen-yang published the artcile< Synthesis of novel thiadiazoles type molecular tweezers based on hyodeoxycholic acid promoted by microwave irradiation>, Electric Literature of 70057-67-9, the main research area is thiadiazole mol tweezer hyodeoxycholic acid microwave preparation.

Ten novel steroidal mol. tweezers are efficiently synthesized via microwave irradiation by using hyodeoxycholic acid as spacer and 1, 3, 4-thiadiazoles unit as arm. Compared with a conventional method, the yields are increased from 38%∼48% to 80%∼91% and the reaction time is reduced from 1800-2400 min to 40-50 min. The structures of these novel mol. tweezers are characterized by 1H NMR, IR, ESI-MS spectra and elemental anal. The recognition properties of these mol. tweezers for D/L-Leu-OMe and D/L-Phe-OMe are investigated by UV-vis spectra. The result indicates that this type of mol. tweezers has good binding properties for D-amino acid Me esters.

Xinan Minzu Daxue Xuebao, Ziran Kexueban published new progress about Complexing agents. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Electric Literature of 70057-67-9.

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

Pau, Amedeo; Catto, Marco; Pinna, Giovanni; Frau, Simona; Murineddu, Gabriele; Asproni, Battistina; Curzu, Maria M.; Pisani, Leonardo; Leonetti, Francesco; Loza, Maria Isabel; Brea, Jose; Pinna, Gerard A.; Carotti, Angelo published the artcile< Multitarget-Directed Tricyclic Pyridazinones as G Protein-Coupled Receptor Ligands and Cholinesterase Inhibitors>, Application of C8H8BrCl, the main research area is tricyclic pyridazinone GPCR ligand cholinesterase inhibitor; AChE inhibitors; BChE inhibitors; GPCR ligands; multitarget-directed ligands; neurodegenerative diseases.

By following a multitarget ligand design approach, a library of 47 compounds was prepared, and they were tested as binders of selected G protein-coupled receptors (GPCRs) and inhibitors of acetyl and/or butyryl cholinesterase. The newly designed ligands feature pyridazinone-based tricyclic scaffolds connected through alkyl chains of variable length to proper amine moieties (e.g., substituted piperazines or piperidines) for GPCR and cholinesterase (ChE) mol. recognition. The compounds were tested at three different GPCRs, namely serotoninergic 5-HT1A, adrenergic α1A, and dopaminergic D2 receptors. Our main goal was the discovery of compounds that exhibit, in addition to ChE inhibition, antagonist activity at 5-HT1A because of its involvement in neuronal deficits typical of Alzheimer’s and other neurodegenerative diseases. Ligands with nanomolar affinity for the tested GPCRs were discovered, but most of them behaved as dual antagonists of α1A and 5-HT1A receptors. Nevertheless, several compounds displaying this GPCR affinity profile also showed moderate to good inhibition of AChE and BChE, thus deserving further investigations to exploit the therapeutic potential of such unusual biol. profiles.

ChemMedChem published new progress about 5-HT1A receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Application of C8H8BrCl.

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

Lee, Ho H.; Denny, William A. published the artcile< An improved synthesis of substituted dibenzo[1,4]dioxines>, Category: chlorides-buliding-blocks, the main research area is catechol cyclocondensation halobenzene; dibenzodioxine.

An improved general synthesis of substituted dibenzo[1,4]dioxines I (R = H, 1-Cl, 2-Cl, 1-NO2, 2-NO2, 1-CO2R1, 2-CO2CHMe2; R1 = H, Me, CHMe2) by reaction of 2-HOC6H4OH and R2C6H3R3R4-1,2 (R2 = H, 3-Cl, 3-NO2, 3-CO2R1, 4-Cl, 4-NO2; R3 = R4 = Cl, F, NO2; R3, R4 = Cl, NO2) with K in HMPA is reported. The yields are generally superior to those in published methods.

Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999) published new progress about Cyclocondensation reaction. 2905-54-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6Cl2O2, Category: chlorides-buliding-blocks.

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