Tag: M.W=250-300

Ghalib, Raza Murad published the artcilePhytochemical analysis, cytotoxic activity and constituents-activity relationships of the leaves of Cinnamomum iners (Reinw. ex Blume-Lauraceae), Related Products of bromides-buliding-blocks, the main research area is Cinnamomum antitumor leaf tumor.

The leaves of Cinnamomum iners (Reinw. ex Blume-Lauraceae) have been refluxed successively with chloroform and alc. to get chloroform extract and alc. extract Both the extracts have been assayed for cytotoxicity against human colorectal tumor cells. The chloroform extract exhibited significant cytotoxicity with IC50 31 μg mL-1 (p < 0.01). However, ethanol extract was found to be much less cytotoxic with IC50 > 200 μg mL-1. The chloroform extract has been further proceeded for chem. anal. by GC-TOFMS and 178 components were identified including acids, amines, amides, aldehydes, alcs., esters, benzene derivatives, bicyclic compounds, terpenes, hydrocarbons, naphthalene derivatives, furan derivatives, azulenes, etc. Nine components representing 51.73% of the total chloroform extract were detected as major components. Caryophyllene (14.41%) and Eicosanoic acid Et ester (12.17%) are the most prominent components of the chloroform extract Components of the chloroform extract β-Caryophyllene (14.41%) as most abundant compound supports potent cytotoxicity as shown by chloroform extract

Natural Product Research published new progress about Antitumor agents. 55099-31-5 belongs to class bromides-buliding-blocks, name is Ethyl 10-bromodecanoate, and the molecular formula is C12H23BrO2, Related Products of bromides-buliding-blocks.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Boutard, Nicolas published the artcileDiscovery and structure-activity relationships of N-aryl 6-aminoquinoxalines as potent PFKFB3 kinase inhibitors, Recommanded Product: 4-Bromo-2-chloro-6-nitroaniline, the main research area is crystal structure neoplasm antitumor PFKFB3 kinase inhibitor aminoquinoxaline; cancer; enzymes; glycolysis; inhibitors; metabolism.

Energy and biomass production in cancer cells are largely supported by aerobic glycolysis in what is called the Warburg effect. The process is regulated by key enzymes, among which phosphofructokinase PFK-2 plays a significant role by producing fructose-2,6-biphosphate; the most potent activator of the glycolysis rate-limiting step performed by phosphofructokinase PFK-1. Herein, the synthesis, biol. evaluation and structure-activity relationship of novel inhibitors of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3), which is the ubiquitous and hypoxia-induced isoform of PFK-2, are reported. X-ray crystallog. and docking were instrumental in the design and optimization of a series of N-aryl 6-aminoquinoxalines. The most potent representative, N-(4-methanesulfonylpyridin-3-yl)-8-(3-methyl-1-benzothiophen-5-yl)quinoxalin-6-amine, displayed an IC50 of 14 nM for the target and an IC50 of 0.49 μM for fructose-2,6-biphosphate production in human colon carcinoma HCT116 cells. This work provides a new entry in the field of PFKFB3 inhibitors with potential for development in oncol.

ChemMedChem published new progress about Antitumor agents. 34033-41-5 belongs to class bromides-buliding-blocks, name is 4-Bromo-2-chloro-6-nitroaniline, and the molecular formula is C6H4BrClN2O2, Recommanded Product: 4-Bromo-2-chloro-6-nitroaniline.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Mueller, Ralf published the artcileLong Hydrocarbon Chain Ether Diols and Ether Diacids That Favorably Alter Lipid Disorders in Vivo, Safety of 1-Bromo-3-(3-bromopropoxy)propane, the main research area is hydrocarbon ether diol diacid lipid structure activity relationship antiobesity.

Long hydrocarbon chain ethers with bis-terminal hydroxyl or carboxyl groups have been synthesized and evaluated for their potential to favorably alter lipid disorders including metabolic syndrome. Compounds were assessed for their effects on the de novo incorporation of radiolabeled acetate into lipids in primary cultures of rat hepatocytes as well as for their effects on lipid and glycemic variables in female obese Zucker fatty rats following 1 and 2 wk of daily oral administration. The most active compounds were found to be sym. with four to five methylene groups separating the central ether functionality and the gem di-Me or methyl/aryl substituents. Biol. activity was found to be greatest for tetramethyl-substituted ether diols, while bis(arylmethyl) derivatives, diethers , and di-Ph ethers were the least active. For the most biol. active compound 28, we observed as much as a 346% increase in serum HDL-cholesterol and a 71% reduction in serum triglycerides at the highest dose administered (100 mg/kg) after 2 wk of treatment. For one compound we observed a 69% reduction in non-HDL-cholesterol, accompanied by a 131% increase in HDL-cholesterol and an 84% reduction in serum triglycerides under the same treatment conditions.

Journal of Medicinal Chemistry published new progress about Antiobesity agents. 58929-72-9 belongs to class bromides-buliding-blocks, name is 1-Bromo-3-(3-bromopropoxy)propane, and the molecular formula is C6H12Br2O, Safety of 1-Bromo-3-(3-bromopropoxy)propane.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Ravindernath, Anisetti published the artcileSynthesis and biological evaluation of benzo[d]imidazolyl chromeno[2,3-d]pyrimidinones, Quality Control of 156089-67-7, the main research area is benzimidazolyl chromenopyrimidinone preparation antibacterial antifungal antioxidant activity SAR.

A series of benzo[d]imidazolyl chromeno[2,3-d]pyrimidnones I (R = H, OMe, Br, Cl, R’ = H; R = R’ =Br) were described. The key intermediate 2-cyano-N-(2-mercapto-1H-benzo[d]imidazol-5-yl)acetamide (II) is obtained by reacting 5-amino-2-mercaptobenzimidazole with Et cyanoacetate. Compound II on reaction with substituted salicylaldehydes afforded 2-imino-N-(2-mercapto-1H-benzo[d]imidazol-5-yl)-2H-chromene-3-carboxamides III (R = H, OMe, Br, Cl, R’ = H; R = R’ =Br) in good yields. Compounds III (R = H, OMe, Br, Cl, R’ = H; R = R’ =Br) on condensation with formalin furnished the title compounds viz., 3-(2-mercapto-1H-benzo[d]imidazol-5-yl)-2H-chromeno[2,3-d]pyrimidin-4(3H)-ones I (R = H, OMe, Br, Cl, R’ = H; R = R’ =Br). All the synthesized compounds were screened for their anti-microbial and anti-oxidant activities.

Medicinal Chemistry Research published new progress about Antibacterial agents. 156089-67-7 belongs to class bromides-buliding-blocks, name is 4,5-Dibromo-2-hydroxybenzaldehyde, and the molecular formula is C7H4Br2O2, Quality Control of 156089-67-7.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Strelyaeva, Angelina V. published the artcileThe study of external signs, microscopy and chemical composition of medicinal plant materials of Verinica beccabunga L. Herb, Quality Control of 55099-31-5, the main research area is external sign microscopy chem composition Verinica beccabunga.

Veronica beccabunga L. belongs to the class dicotyledons, order Lamiáles, family Scrophulariaceae. Representatives of the genus Veronica have long been used in folk medicine as antiinflammatory, antibacterial, antiseptic, wound healing, hemostatic, choleretic and antispasmodic drugs. Widely studied species are Veronica officinalis and Veronica chamaedrys. Veronica beccabunga L., which is the object of our study, remains a poorly studied plant. The study of external signs, microscopy and chem. composition of medicinal plant materials of Veronica beccabunga L. herb. Chromato-mass spectrometry was used in the work. When describing external signs and microscopy, diagnostic signs of Veronica beccabunga were revealed. 27 compounds were identified by chromatog.-mass spectrometry. The maximum content falls on: Citronellol epoxide (R or S) (30.5%), Linolenic acid, Et ester (15.18), Di-Et succinate (12.17%), Et palmitate (6.43%), Phytol (4.89%), Acetaldehyde Et amyl acetal (3.94%), Dibenzylamine (3.01%), Oleamide (2.77%), 2-(1-Methylbutyl)oxirane (2.7%), Bu octyl phthalate(1.7%), Et 10-bromodecanoate (1.68), Valeric acid, 4-methyl-, Et ester (1.58), Glycoside detected : 1-Benzyl-1H-benzimidazole 3-oxide (0.76%). The revealed morphol. and anatomical signs of Veronica beccabunga herb can be used to diagnose this species and develop authenticity indicators for promising medicinal herbs. 27 compounds were identified by chromatographymass spectrometry. Using the method of simple normalization, the relative percentage of identified compounds was determined

Pharmacognosy Journal published new progress about Anti-inflammatory agents. 55099-31-5 belongs to class bromides-buliding-blocks, name is Ethyl 10-bromodecanoate, and the molecular formula is C12H23BrO2, Quality Control of 55099-31-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Murray, Michael published the artcileCarbon Chain Length Modulates MDA-MB-231 Breast Cancer Cell Killing Mechanisms by Mitochondrially Targeted Aryl-Urea Fatty Acids, Related Products of bromides-buliding-blocks, the main research area is aryl urea fatty acid preparation structure breast cancer mitochondrion; antitumor agents; apoptosis; breast cancer; fatty acids; lipid drugs.

Targeting the tumor cell mitochondrion could produce novel anticancer agents. We designed an aryl-urea fatty acid (1 g; 16({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)hexadecanoic acid) that disrupted the mitochondrion and decreased MDA-MB-231 breast cancer cell viability. To optimize the aryl-ureas the present study evaluated mitochondrial targeting by 1 g analogs containing alkyl chains between 10-17 carbons. Using the dye JC-1, the C12-C17 analogs efficiently disrupted the mitochondrial membrane potential (IC50s 3.5±1.2 to 7.6±1.1μM) and impaired ATP production; shorter analogs were less active. 7-Aminoactinomycin D/annexin V staining and flow cytometry showed that these agents activated the killing mechanisms of necrosis and apoptosis to varying extents (7-aminoactinomycin D/annexin V staining ratios 4.3-6.0). Indeed, 1 g and its C17 analog preferentially activated necrosis and apoptosis, resp. (ratios 2.1 and 16). Taken together, alkyl chain length is a determinant of mitochondrial targeting by aryl-ureas and can be varied to develop analogs that activate apoptosis or necrosis in a regulated fashion.

ChemMedChem published new progress about Antiproliferative agents. 55099-31-5 belongs to class bromides-buliding-blocks, name is Ethyl 10-bromodecanoate, and the molecular formula is C12H23BrO2, Related Products of bromides-buliding-blocks.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhang, Xuan published the artcileDiscovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity, Related Products of bromides-buliding-blocks, the main research area is preparation PROTAC apoptosis BCLxL degrader cancer platelet toxicity; Apoptosis; BCL-X(L); Degradation; PROTAC; Platelet.

Anti-apoptotic protein BCL-XL plays a key role in tumorigenesis and cancer chemotherapy resistance, rendering it an attractive target for cancer treatment. However, BCL-XL inhibitors such as ABT-263 cannot be safely used in the clinic because platelets solely depend on BCL-XL to maintain their viability. To reduce the on-target platelet toxicity associated with the inhibition of BCL-XL, we designed and synthesized PROTAC BCL-XL degraders that recruit CRBN or VHL E3 ligase because both of these enzymes are poorly expressed in human platelets compared to various cancer cell lines. We confirmed that platelet-toxic BCL-XL/2 dual inhibitor ABT-263 can be converted into platelet-sparing CRBN/VHL-based BCL-XL specific degraders. A number of BCL-XL degraders are more potent in killing cancer cells than their parent compound ABT-263. Specifically, XZ739, a CRBN-dependent BCL-XL degrader, is 20-fold more potent than ABT-263 against MOLT-4 T-ALL cells and has >100-fold selectivity for MOLT-4 cells over human platelets. Our findings further demonstrated the utility of PROTAC technol. to achieve tissue selectivity through recruiting differentially expressed E3 ligases.

European Journal of Medicinal Chemistry published new progress about Antitumor agents (low). 55099-31-5 belongs to class bromides-buliding-blocks, name is Ethyl 10-bromodecanoate, and the molecular formula is C12H23BrO2, Related Products of bromides-buliding-blocks.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Tron, Arnaud published the artcileReversible Photocapture of a [2]Rotaxane Harnessing a Barbiturate Template, COA of Formula: C12H23BrO2, the main research area is reversible photocapture rotaxane barbiturate template.

Photoirradiation of a hydrogen-bonded mol. complex comprising acyclic components, namely, a stoppered thread (1) with a central barbiturate motif and an optimized doubly anthracene-terminated acyclic Hamilton-like receptor (2b), leads to an interlocked architecture, which was isolated and fully characterized. The sole isolated interlocked photoproduct (Φ = 0.06) is a [2]rotaxane, with the dimerized anthracenes assuming a head-to-tail geometry, as evidenced by NMR spectroscopy and consistent with mol. simulation, physicochem., physicochem. (PM6). A different behavior was observed on irradiating homologous mol. complexes 1⊂2a, 1⊂2b, and 1⊂2c, where the spacers of 2a, 2b, and 2c incorporated 3, 6, and 9 methylene units, resp. While no evidence of interlocked structure formation was observed following irradiation of 1⊂2a, a kinetically labile rotaxane was obtained on irradiating the complex 1⊂2c, and ring slippage was revealed. A more stable [2]rotaxane was formed on irradiating 1⊂2b, whose capture is found to be fully reversible upon heating, thereby resetting the system, with some fatigue (38%) after four irradiation-thermal reversion cycles.

Journal of Organic Chemistry published new progress about [2+2] Photocycloaddition reaction. 55099-31-5 belongs to class bromides-buliding-blocks, name is Ethyl 10-bromodecanoate, and the molecular formula is C12H23BrO2, COA of Formula: C12H23BrO2.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Ambartsumova, R. F. published the artcileOn interaction of 2-aminobenzothiazoles with halohydrins, Application of 1-Bromo-3-(3-bromopropoxy)propane, the main research area is benzothiazolamine halohydrin alkylation oxidation dimerization; iminobenzothiazoline preparation; benzothiazolylideneammonium chloride preparation.

On heating on a boiling water bath, 2-aminobenzothiazoles react with Cl(CH2)2OH to yield mainly the corresponding 3-(2-chloroethyl)benzothiazolin-2-ones. Reducing the reaction temperature increases the fraction of 2-imino-3-(2-hydroxyethyl)benzothiazolines. In both instances, formation of bis[3-(2-hydroxyethyl)benzothiazol-2-ylidene]ammonium chlorides is observed The reaction of 2-aminobenzothiazole with Br(CH2)3OH gives only the corresponding amino alcs. The anomalous products from the reaction of β-chloroethyl derivatives of benzothiazolinones result from a dominating side-reaction of the starting 2-aminobenzothiazoles with the Cl(CH2)2OH thermolysis products that are formed on boiling.

Chemistry of Heterocyclic Compounds (New York)(Translation of Khimiya Geterotsiklicheskikh Soedinenii) published new progress about Halohydrins Role: RCT (Reactant), RACT (Reactant or Reagent). 58929-72-9 belongs to class bromides-buliding-blocks, name is 1-Bromo-3-(3-bromopropoxy)propane, and the molecular formula is C6H12Br2O, Application of 1-Bromo-3-(3-bromopropoxy)propane.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Cristau, Henri-Jean published the artcileSynthesis of diphosphine dioxides for extraction of actinides using supported liquid membranes technology, COA of Formula: C6H12Br2O, the main research area is diphosphine dioxide preparation extraction actinide; organophosphorus extractant diphosphine dioxide preparation; radioactive liquid waste treatment organophosphorus extractant; plutonium extraction diphosphine dioxide; neptunium extraction diphosphine dioxide; supported liquid membrane actinide extraction organophosphorus.

A recurrent method for synthesis of diphosphine dioxides to be used for extraction of actinides from acidic aqueous solution is described. Selective phosphonium salt formation and cleavage permits the stepwise introduction of different bridges between the P atoms as well as various chains on them. The influence of the structural parameters on liquid-liquid extraction properties of Pu, Np, and Am was studied. Pu and Np can be efficiently removed from radioactive contaminated liquid wastes, using the supported liquid membranes technol. with the more lipophilic organophosphorus extractants, e.g., I.

Heteroatom Chemistry published new progress about Actinides Role: REM (Removal or Disposal), PROC (Process). 58929-72-9 belongs to class bromides-buliding-blocks, name is 1-Bromo-3-(3-bromopropoxy)propane, and the molecular formula is C6H12Br2O, COA of Formula: C6H12Br2O.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary