Tag: M.W=200-250

Di Matteo, Mauro published the artcileSynthesis and biological characterization of 3-(imidazol-1-ylmethyl)piperidine sulfonamides as aromatase inhibitors, Category: chlorides-buliding-blocks, the main research area is imidazolylmethylpiperidine sulfonamide preparation aromatase inhibitor; Anticancer agents; Aromatase inhibitor; Imidazole; Sulfonamide; Synthesis.

The most frequently used treatment for hormone receptor pos. breast cancer in post-menopausal women are aromatase inhibitors. In order to develop new aromatase inhibitors, we designed and synthesized new imidazolylmethylpiperidine sulfonamides using the structure of the previously identified aromatase inhibitor SYN 20028567 as starting lead. By this approach, three new aromatase inhibitors with IC50 values that are similar to that of letrozole and SYN 20028567 were identified.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Category: chlorides-buliding-blocks.

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

Yan, Luping published the artcileStructure-Activity Relationships for the Marine Natural Product Sintokamides: Androgen Receptor N-Terminus Antagonists of Interest for Treatment of Metastatic Castration-Resistant Prostate Cancer, Application of Methyl 4,4,4-trichlorobutanoate, the main research area is marine sintokamide androgen receptor antagonist prostate cancer antitumor preparation.

Synthetic analogs of the marine natural product sintokamides have been prepared in order to investigate the structure-activity relationships for the androgen receptor N-terminal domain (AR NTD) antagonist activity of the sintokamide scaffold. An in vitro LNCaP cell-based transcriptional activity assay with an androgen-driven luciferase (Luc) reporter was used to monitor the potency of analogs. The data have shown that the chlorine atoms on the leucine side chains are essential for potent activity. Analogs missing the nonchlorinated Me groups of the leucine side chains (C-1 and C-17) are just as active and in some cases more active than the natural products. Analogs with the natural R configuration at C-10 and the unnatural R configuration at C-4 are most potent. Replacing the natural propionamide N-terminus cap with the more sterically hindered pivaloylamide N-terminus cap leads to enhanced potency. The tetramic acid fragment and the Me ether on the tetramic acid fragment are essential for activity. The SAR optimized analog 76 is more selective, easier to synthesize, more potent, and presumed to be more resistant to proteolysis than the natural sintokamides.

Journal of Natural Products published new progress about Antitumor agents. 19376-57-9 belongs to class chlorides-buliding-blocks, name is Methyl 4,4,4-trichlorobutanoate, and the molecular formula is C5H7Cl3O2, Application of Methyl 4,4,4-trichlorobutanoate.

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

Dickens, Michael P. published the artcile5-Deazaflavin derivatives as inhibitors of p53 ubiquitination by HDM2, Application In Synthesis of 93118-03-7, the main research area is deazaflavin derivative preparation p53 ubiquitination inhibitor SAR; Cancer; Deazaflavin; HDM2–p53; Ubiquitin E3 ligase; Ubiquitination inhibitors.

Based on previous reports of certain 5-deazaflavin derivatives being capable of activating the tumor suppressor p53 in cancer cells through inhibition of the p53-specific ubiquitin E3 ligase HDM2, we have conducted an structure-activity relation (SAR) anal. through systematic modification of the 5-deazaflavin template. This anal. shows that HDM2-inhibitory activity depends on a combination of factors. The most active compounds (e.g., I) contain a trifluoromethyl or chloro substituent at the deazaflavin C9 position and this activity depends to a large extent on the presence of at least one addnl. halogen or Me substituent of the Ph group at N10. Our SAR results, in combination with the HDM2 RING domain receptor recognition model we present, form the basis for the design of drug-like and potent activators of p53 for potential cancer therapy.

Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Application In Synthesis of 93118-03-7.

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

Shono, Tatsuya published the artcileFormation of a reasonably stabilized trichloromethyl anion by the reaction of chloroform with electrogenerated base and its 1,4-addition to α,β-unsaturated carbonyl compounds, Recommanded Product: Methyl 4,4,4-trichlorobutanoate, the main research area is addition anion chloromethyl unsaturated carboxylate nitrile; ammonium tetraalkyl electrochem reduction pyrrolidinone; chloromethyl anion addition unsaturated carboxylate nitrile; carboxylate unsaturated addition chloromethyl anion; cyclopropanation chloroacetate anion; electrochem reduction pyrrolidinone tetraalkylammonium; nitrile unsaturated addition chloromethyl anion; pyrrolidinone reduction electrochem tetraalkylammonium; reduction electrochem pyrrolidinone tetraalkylammonium.

Electrochem. reduction of 2-pyrrolidinone in the presence of tetraalkylammonium salts gave the resp. tetraalkylammonium salts with pyrrolidinone. The latter reacted with CHCl3 to give Cl3C-, which underwent addition reactions with α,β-unsaturated carboxylates or nitriles. Thus, reaction of Cl2CHCO2Me in the presence of tetraalkylammonium salts with pyrrolidinone gave di-Me 1-chloro-1,2-cyclopropanedicarboxylates. Addition of CHCl3 to CH2:CHCO2Me in the presence of the tetraethylammonium-pyrrolidinone salt gave 87% Cl3CCH2CH2CO2Me.

Tetrahedron Letters published new progress about Addition reaction. 19376-57-9 belongs to class chlorides-buliding-blocks, name is Methyl 4,4,4-trichlorobutanoate, and the molecular formula is C5H7Cl3O2, Recommanded Product: Methyl 4,4,4-trichlorobutanoate.

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

Hobson, Adrian D. published the artcileDiscovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders, Application of 4-(4-Chlorophenoxy)benzaldehyde, the main research area is sphingosine phosphate receptor agonist neurodegenerative disorder.

S1P5 is one of 5 receptors for sphingosine-1-phosphate and is highly expressed on endothelial cells within the blood-brain barrier, where it maintains barrier integrity in in vitro models. Little more is known about the effects of S1P5 modulation due to the absence of tool mols. with suitable selectivity and drug-like properties. We recently reported that mol. A-971432 (Harris, 2010) (29 in this paper) is highly efficacious in reversing lipid accumulation and age-related cognitive decline in rats. Herein we describe the development of a series of selective S1P5 agonists that led to the identification of compound 29, which is highly selective for S1P5 and has excellent plasma and CNS exposure after oral dosing in preclin. species. To further support its suitability for in vivo studies of S1P5 biol., we extensively characterized 29, including confirmation of its selectivity in pharmacodynamic assays of S1P1 and S1P3 function in rats. In addition, we found that 29 improves blood-brain barrier integrity in an in vitro model and reverses age-related cognitive decline in mice. These results suggest that S1P5 agonism is an innovative approach with potential benefit in neurodegenerative disorders involving lipid imbalance and/or compromised blood-brain barrier such as Alzheimer’s disease or multiple sclerosis.

Journal of Medicinal Chemistry published new progress about Alzheimer disease. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Application of 4-(4-Chlorophenoxy)benzaldehyde.

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

Wu, Junchen published the artcileA Molecular Peptide Beacon for the Ratiometric Sensing of Nucleic Acids, Name: Pyrene-2-carboxylic acid, the main research area is mol peptide beacon preparation ratiometry fluorescence sensor DNA.

A pyrene-functionalized cationic oligopeptide I efficiently binds to double-stranded DNA, as shown by different spectrophotochem. studies. Upon binding, the conformation of I changes from a folded to an extended form, which leads to a distinct change in the fluorescence properties. Thus, I functions as a mol. peptide beacon, and as it is easily taken up by cells, I can also be used for imaging of nucleic acids within cells.

Journal of the American Chemical Society published new progress about Biological uptake. 36428-96-3 belongs to class chlorides-buliding-blocks, name is Pyrene-2-carboxylic acid, and the molecular formula is C17H10O2, Name: Pyrene-2-carboxylic acid.

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

Schneider, Joanne published the artcileDegradation of pyrene, benz[a]anthracene, and benzo[a]pyrene by Mycobacterium sp. strain RJGII-135, isolated from a former coal gasification site, Related Products of chlorides-buliding-blocks, the main research area is Mycobacterium metabolism pyrene benzanthracene benzopyrene pollutant.

The degradation of three polycyclic aromatic hydrocarbons (PAH), pyrene (PYR), benz[a]anthracene (BAA), and benzo[a]pyrene (BaP), by Mycobacterium sp. strain RJGII-135 was studied. The bacterium was isolated from an abandoned coal gasification site soil by analog enrichment techniques and found to mineralize [14C]PYR. Further degradation studies with PYR showed three metabolites formed by Mycobacterium sp. strain RJGII-135, including 4,5-phenanthrenedicarboxylic acid not previously isolated, 4-phenanthrenecarboxylic acid, and 4,5-pyrenedihydrodiol. At least two dihydrodiols, 5,6-BAA-dihydrodiol and 10,11-BAA-dihydrodiol, were confirmed by high-resolution mass spectral and fluorescence analyses as products of the biodegradation of BAA by Mycobacterium sp. strain RJGII-135. Addition, a cleavage product of BAA was also isolated. Mass spectra and fluorescence data support two different routes for the degradation of BaP by Mycobacterium sp. strain RJGII-135. The 7,8-BaP-dihydrodiol and three cleavage products of BaP, including 4,5-chrysenedicarboxylic acid and a dihydropyrenecarboxylic acid metabolite, have been isolated and identified as degradation products formed by Mycobacterium sp. strain RJGII-135. These latter results represent the first example of the isolation of BaP ring fission products formed by a bacterial isolate. We propose that while this bacterium appears to attack only one site of the PYR mol., it is capable of degrading different sites of the BAA and BaP mols., and although the sites of attack may be different, the ability of this bacterium to degrade these PAH is well supported. The proposed pathways for biodegradation of these compounds by this Mycobacterium sp. strain RJGII-135 support the dioxygenase enzymic processes reported previously for other bacteria. Microorganisms like Mycobacterium sp. strain RJGII-135 will be invaluable in attaining the goal of remediation of sites containing mixtures of these PAH.

Applied and Environmental Microbiology published new progress about Coal gasification. 36428-96-3 belongs to class chlorides-buliding-blocks, name is Pyrene-2-carboxylic acid, and the molecular formula is C17H10O2, Related Products of chlorides-buliding-blocks.

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

Ram, Ram N. published the artcileCopper(I)-Promoted Synthesis of Highly Substituted and Functionalized Tetrahydrothiophenes, Recommanded Product: Methyl 4,4,4-trichlorobutanoate, the main research area is radical cyclization trihaloethyl allyl sulfide; tetrahydrothiophene stereoselective preparation; thiophene tetrahydro stereoselective preparation.

Copper(I)-promoted 5-exo halogen-atom-transfer radical cyclization of 2,2,2-trihaloethyl allyl sulfides gave highly functionalized tetrahydrothiophenes in good to high yields. Stereochem. aspects of the diastereomeric mixtures of products formed under different reaction conditions were evaluated, and single crystal diffraction anal. and 2D NMR spectroscopic anal. were carried out. The synthetic application of α-acetoxytetrahydrothiophenes in the preparation of a dihydrothiophene has also been demonstrated.

European Journal of Organic Chemistry published new progress about Crystal structure. 19376-57-9 belongs to class chlorides-buliding-blocks, name is Methyl 4,4,4-trichlorobutanoate, and the molecular formula is C5H7Cl3O2, Recommanded Product: Methyl 4,4,4-trichlorobutanoate.

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

Cabral, Lilia I. L. published the artcileSynthesis and structure of 2-substituted pyrene-derived scaffolds, Safety of Pyrene-2-carboxylic acid, the main research area is functionalized pyrene synthesis tetrahydropyrene intermediate.

Pyrenes bear a propensity to form fluorescent excimers, and thus this chromophore is often found in sensors and fluorescent probes. 2-Functionalized pyrenes are of particular interest, however the preparation of these scaffolds is not trivial, involving synthetic routes that require 4,5,9,10-tetrahydropyrene as a key intermediate. Herein, the development and optimization of routes for the synthesis of 2-functionalized pyrene-derived building blocks, with potential to be used as tags in the preparation of fluorescent probes, is described. Addnl., the crystal structures of Et 4,5,9,10-tetrahydro-2-pyrene-5-oxopentanoate and 2-acetyl-4,5,9,10-tetrahydropyrene revealed distinct conformations of the saturated tetrahydropyrene rings.

Tetrahedron Letters published new progress about Crystal structure. 36428-96-3 belongs to class chlorides-buliding-blocks, name is Pyrene-2-carboxylic acid, and the molecular formula is C17H10O2, Safety of Pyrene-2-carboxylic acid.

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

Wang, Lijiao published the artcileStable Double and Quadruple [5]Helicene Derivatives: Synthesis, Structural Analysis, and Physical Properties, Application In Synthesis of 3032-32-4, the main research area is pyrene fused indenofluoranthene helicene preparation crystal structure; UV visible spectra lack fluorescence pyrene fused indenofluoranthene helicene; reduction oxidation potential pyrene fused indenofluoranthene helicene.

Pyrene-fused indenofluoranthene helicenes I and II were prepared; the crystal structure of I and the photophys. properties, and oxidation and reduction potentials of I and II were determined Stereoisomerization of the enantiomers and diastereomers of I and II were studied computationally. Chem. oxidation of II with NO+BF4- generated radical cation species at ambient temperature

Organic Letters published new progress about Crystal structure. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, Application In Synthesis of 3032-32-4.

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