Month: October 2022

Fioravanti, Rossella; Tomassi, Stefano; Bello, Elisabetta Di; Romanelli, Annalisa; Plateroti, Andrea Maria; Benedetti, Rosaria; Conte, Mariarosaria; Novellino, Ettore; Altucci, Lucia; Valente, Sergio; Mai, Antonello published the artcile< Properly substituted cyclic bis-(2-bromobenzylidene) compounds behaved as dual p300/CARM1 inhibitors and induced apoptosis in cancer cells>, Reference of 17082-09-6, the main research area is cyclic bisbromobenzylidene compound preparation diastereoselective antitumor activity; drug discovery; epigenetics; histone acetylation; histone methylation; multi-target agents.

The 1-benzyl-3,5-bis((E)-3-bromobenzylidene)piperidin-4-one displayed dual p300/EZH2 inhibition joined to cancer-selective cell death in a panel of tumor cells and in in-vivo xenograft models, a series of bis((E)-2-bromobenzylidene) cyclic compounds I (X = CH2) and I (X is NR, where R = H, Me, Bn, etc.) were prepared to test in biochem. (p300, PCAF, SIRT1/2, EZH2, and CARM1) and cellular (NB4, U937, MCF-7, SH-SY5Y) assays. The majority of I exhibited potent dual p300 and CARM1 inhibition, sometimes reaching the submicromolar level, and induction of apoptosis mainly in the tested leukemia cell lines. The most effective compounds in both enzyme and cellular assays carried a 4-piperidone moiety and a Me, benzyl, or acyl substituent at N1 position I [X is NR, where R = H, Me, Bn, 2-oxo-2-phenylethyl, 2-oxo-3-phenylpropyl, 2-oxo-4-phenylbutyl]. Elongation of the benzyl portion to I [X is NR, where R = 2-phenylethyl, 3-phenylpropyl] decreased the potency of compounds at both the enzymic and cellular levels, but the activity was promptly restored by introduction of a ketone group into the phenylalkyl substituent I [X is NR, where R = 2-oxo-2-phenylethyl, 3-oxo-3-phenylpropyl, 4-oxo-4-phenylbutyl]. Western blot analyses performed in NB4 and MCF-7 cells on selected compounds confirmed their inhibition of p300 and CARM1 through decrease of the levels of acetyl-H3 and acetyl-H4, marks for p300 inhibition, and of H3R17me2, mark for CARM1 inhibition.

Molecules 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, Reference of 17082-09-6.

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

Molchanov, A. P.; Pecheritsyna, Ya. P.; Kostikov, R. R. published the artcile< Synthesis and thermal transformations of adducts of dihalocarbenes with cyclopentadiene and spiro[2.4]hepta-4,6-diene dimers>, Safety of 3-Chlorophenethyl Bromide, the main research area is cyclopentadiene dimer cyclopropanation dihalocarbene; spiroheptadiene dimer cyclopropanation dihalocarbene; tetracycloundecene dihalo preparation thermolysis; cyclopropanespirotetracycloundecenespirocyclopropane dihalo preparation thermolysis.

Reaction of the title dimers with CHCl3 or with CHBrXY (X = Y = Br; X, Y = Cl, Br; X = F, Y = Br) in hexane containing KOCMe3 gave 12-33% cyclopropanated adducts I and II (X = Y = Cl, Br; X = Y = Cl, Br; X = F, Y = Br). Thermal decomposition of I gave tricyclic dihalo compounds III via ring cleavage, whereas II gave 62-73% 3-XC6H4CH2CH2Y by a retro-Diels-Alder route.

Zhurnal Organicheskoi Khimii published new progress about Cyclopropanation. 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Safety of 3-Chlorophenethyl Bromide.

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

Chang, Chia-Lin; Wu, Chin-Sheng; Wang, Sen-Wen; Wang, Jih-Pyang published the artcile< Synthesis and biological activity of 5-(2'-alkoxycarbonyl substituted phenoxy)furan-2-carboxylic acid derivatives>, SDS of cas: 22717-55-1, the main research area is alkoxycarbonylphenoxyfurancarboxylic acid derivative synthesis biol activity antiallergic antiinflammatory.

A series of 5-(2′-alkoxycarbonyl substituted phenoxy)furan-2-carboxylic acid derivatives were prepared by a facile synthetic route: reaction of Et 5-nitro-2-furoate with the corresponding salicylates. None of the compounds inhibited PMA-induced neutrophil superoxide formation. On the contrary, some carboxylates significantly inhibited fMLP-induced neutrophil degranulation with much greater activity than the pos. control, TFP. One compound also inhibited superoxide formation. Furthermore, another compound strongly inhibited β-glucuronidase and histamine release from mast cells. In particular, this compound was shown to be a novel lead compound with excellent anti-allergic and anti-inflammatory activities. The other compound was shown to be a novel lead compound with excellent anti-inflammatory activity.

Chinese Pharmaceutical Journal (Taipei, Taiwan) published new progress about Allergy. 22717-55-1 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO3, SDS of cas: 22717-55-1.

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

Liu, Jiwen; Fu, Zice; Wang, Yingcai; Schmitt, Mike; Huang, Alan; Marshall, Derek; Tonn, George; Seitz, Lisa; Sullivan, Tim; Lucy Tang, H.; Collins, Tassie; Medina, Julio published the artcile< Discovery and optimization of CRTH2 and DP dual antagonists>, Name: 3-Chloro-4-methylbenzene-1-sulfonyl chloride, the main research area is phenylacetic acid derivative preparation prostanoid CRTH2 DP dual antagonist.

A series of phenylacetic acid derivatives was discovered as CRTH2 antagonists. Modification of the series led to compounds that are also antagonists of DP. Since activation of CRTH2 and DP are believed to play key roles in mediating responses of asthma and other immune diseases, this series was optimized to increase the dual antagonistic activities and improve pharmacokinetic properties. These efforts led to selection of AMG 009 as a clin. candidate.

Bioorganic & Medicinal Chemistry Letters published new progress about Antiasthmatics. 42413-03-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O2S, Name: 3-Chloro-4-methylbenzene-1-sulfonyl chloride.

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

Warner, Andrew J.; Lawson, James R.; Fasano, Valerio; Ingleson, Michael J. published the artcile< Formation of C(sp2)-boronate esters by borylative cyclization of alkynes using BCl3>, Quality Control of 16799-05-6, the main research area is cyclization borylative alkyne aryl boron trichloride preparation cyclic alkenylboronate; fluorenyl azafluorenyl boronate preparation dipropargyl compound cyclization boron trichloride; intramol borylation arylalkyne arene boron trichloride preparation diaryl vinylboronate; alkynes; boron; cyclizations; heterocycles; synthetic methods.

Arylpropargyl compounds R1C6H4YCH2CCR2 undergo cyclization in a reaction with BCl3 and pinacol, yielding cyclic alkenylboronates I (2, R1 = H, Me, MeO, Cl; Y = CH2, NTs, O; R2 = Ph, ClC6H4, C6F5, 3-CF3C6H4, 4-NCC6H4, MeC6H4, Br, Me, 1-naphthyl, PhCH:CH, 4-NO2C6H4, 4-EtO2CC6H4). Diynes R3CCCH2YCH2CCR3 gave boronates II (R3 = Ph, 10a,b; Y = CH2, NTs) or III (11, R3 = H, Y = CH2). BCl3 is an inexpensive electrophile which induces the borylative cyclization of a wide range of substituted alkynes to regioselectively form polycycles containing synthetically versatile C(sp2)-boronate esters. It proceeds rapidly, with good yields and is compatible with a range of functional groups and substitution patterns. Intermol. 1,2-carboboration of alkynes Ar1CCMe is also achieved using BCl3 and arene Ar2H to generate trisubstituted vinyl boronate esters Ar1Ar2C:CMe(Bpin) (12, Ar1 = Ph, Ar2 = 5-methyl-2-thienyl).

Angewandte Chemie, International Edition published new progress about Alkynes, aryl Role: RCT (Reactant), RACT (Reactant or Reagent). 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

Lindsley, Craig W.; Zhao, Zhijian; Leister, William H.; O’Brien, Julie; Lemaire, Wei; Williams, David L. Jr.; Chen, Tsing-Bau; Chang, Raymond S. L.; Burno, Maryann; Jacobson, Marlene A.; Sur, Cyrille; Kinney, Gene G.; Pettibone, Douglas J.; Tiller, Philip R.; Smith, Sheri; Tsou, Nancy N.; Duggan, Mark E.; Conn, P. Jeffrey; Hartman, George D. published the artcile< Design, synthesis, and in vivo efficacy of glycine transporter-1 (GlyT1) inhibitors derived from a series of [4-phenyl-1-(propylsulfonyl)piperidin-4-yl]methyl benzamides>, Quality Control of 162046-61-9, the main research area is antipsychotic piperidinylmethylbenzamide preparation SAR glycine transporter.

An iterative analog library synthesis approach was employed to develop SAR for the title compounds Analog I was thus identified as a novel, centrally active GlyT1 inhibitor. I enhanced prepulse inhibition in a rodent behavioral model sensitive to antipsychotic treatment.

ChemMedChem published new progress about Antipsychotics. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Quality Control of 162046-61-9.

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

Zhou, Yan; Zhou, Zebiao; Liu, Siqi; Cai, Mingzhong published the artcile< Recyclable palladium-catalyzed cyclocarbonylation between benzyl chlorides and salicylic aldehydes towards coumarins>, Electric Literature of 611-19-8, the main research area is silica immobilized bidentate phosphine palladium complex preparation; salicylic aldehyde aralkyl chloride palladium catalyst cyclocarbonylation; coumarin preparation.

A novel and practical route to coumarin derivatives was developed via the heterogeneous Pd-catalyzed carbonylative reaction and subsequent intramol. condensation process starting from com. easily available benzyl chlorides and salicylic aldehydes. Reactions were performed in the existence of 2 mol% of an SBA-15-immobilized bidentate phosphine palladium complex [SBA-15-P,P-PdCl2] in dioxane at 110°C with Et3N as base under 10 bar of CO to afford a wide range of coumarin derivatives mostly with good to high yields. Importantly, this new heterogenized palladium complex was easy to recover via filtration of the reaction mixture, and was recyclable up to 8 times without apparent drop in its catalytic performance.

Molecular Catalysis published new progress about Aralkyl chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 611-19-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2, Electric Literature of 611-19-8.

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

Nishimura, Yoko; Morikawa, Yuji; Kondo, Chiaki; Tonomura, Yutaka; Fukushima, Ryou; Torii, Mikinori; Uehara, Takeki published the artcile< Genomic biomarkers for cardiotoxicity in rats as a sensitive tool in preclinical studies>, HPLC of Formula: 6055-19-2, the main research area is isoproterenol hydrochloride cyclosporin A Spp1 gene biomarker; cardiac troponin; cardiotoxicity; drug development; genomic biomarker; toxicogenomics.

The development of safer drugs is a high priority for pharmaceutical companies. Among the various toxicities caused by drugs, cardiotoxicity is an important issue because of its lethality. In addition, cardiovascular toxicity leads to the attrition of many drug candidates in both preclin. and clin. phases. Although histopathol. and blood chem. examinations are the current gold standards for detecting cardiotoxicity in preclin. studies, the large number of withdrawals from clin. studies owing to safety problems indicate that a more sensitive tool is required. We recently identified 32 genes that were candidate genomic biomarkers for cardiotoxicity in rats. Based on their functions, the present study focused on 8 of these 32 genes (Spp1, Fhl1, Timp1, Serpine1, Bcat1, Lmcd1, Rnd1 and Tgfb2). Diagnostic accuracy for the genes was determined by a receiver-operating characteristic (ROC) anal. using more cardiotoxic and non-cardiotoxic compounds In addition, an optimized support vector machine (SVM) model that was composed of Spp1 and Timp1 was newly constructed. This new multi-gene model exhibited a much higher diagnostic accuracy than that observed for plasma cardiac troponin I (cTnI), which is one of the most useful plasma biomarkers for cardiotoxicity detection. Furthermore, we determined that this multi-gene model could predict potential cardiotoxicity in rats in the absence of any cardiac histopathol. lesions or elevations of plasma cTnI. Overall, this multi-gene model exhibited advantages over classic tools commonly used for cardiotoxicity evaluations in rats. Our current results suggest that application of the model could potentially lead to the production of safer drugs. Copyright © 2013 John Wiley & Sons, Ltd.

Journal of Applied Toxicology published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (Bcat1). 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, HPLC of Formula: 6055-19-2.

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