Category: bromides-buliding-blocks

Melin, Lea published the artcileDevelopment of LM98, a Small-Molecule TEAD Inhibitor Derived from Flufenamic Acid, Quality Control of 647020-71-1, the main research area is anticancer agent cell migration TEAD LM98 flufenamic acid; Flufenamic acid; Hippo pathway; SAR; TEAD; palmitic acid.

The YAP-TEAD transcriptional complex is responsible for the expression of genes that regulate cancer cell growth and proliferation. Dysregulation of the Hippo pathway due to overexpression of TEAD has been reported in a wide range of cancers. Inhibition of TEAD represses the expression of associated genes, demonstrating the value of this transcription factor for the development of novel anti-cancer therapies. We report herein the design, synthesis and biol. evaluation of LM98, a flufenamic acid analog. LM98 shows strong affinity to TEAD, inhibits its autopalmitoylation and reduces the YAP-TEAD transcriptional activity. Binding of LM98 to TEAD was supported by 19F-NMR studies while co-crystallization experiments confirmed that LM98 is anchored within the palmitic acid pocket of TEAD. LM98 reduces the expression of CTGF and Cyr61, inhibits MDA-MB-231 breast cancer cell migration and arrests cell cycling in the S phase during cell division.

ChemMedChem published new progress about Antitumor agents. 647020-71-1 belongs to class bromides-buliding-blocks, name is Methyl 2-bromo-3-fluorobenzoate, and the molecular formula is C8H6BrFO2, Quality Control of 647020-71-1.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

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

Kuo, Gee-Hong published the artcileSynthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors, Computed Properties of 41668-13-7, the main research area is pyridinyltin dichloropyrazine Stille coupling; chloropyrazine pyridine preparation; pyrazine pyridine derivative preparation VEGFR2 ligand; pyridine pyrazine derivative preparation anticancer.

There is much evidence that direct inhibition of the kinase activity of vascular endothelial growth factor receptor-2 (VEGFR-2) will result in the reduction of angiogenesis and the suppression of tumor growth. Palladium-catalyzed C-C bond, C-N bond formation reactions were used to assemble various pyrazine-pyridine biheteroaryls as potent VEGFR-2 inhibitors. Among them, I [R = NH(CH2)4OH, NH(CH2)2NMe2] exhibited the highest kinase selectivity against fibroblast growth factor receptor kinase, platelet-derived growth factor receptor kinase, and glycogen synthase kinase-3. All of these compounds showed good cellular potency to inhibit VEGF-stimulated proliferation of human umbilical vein endothelial cells (HUVEC) but with modest effects on the unstimulated growth of HUVEC. The low inhibition of these compounds to the growth of tumor cell lines, such as HeLa, HCT-116, and A375 further confirms that these VEGFR-2 inhibitors are not cytotoxic agents. The in vivo antitumor activity of I were demonstrated in the A375 human melanoma xenograft nude mice model. Mol. modeling (QSAR anal.) was conducted in an attempt to rationalize the observed structure-activity relationship.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 41668-13-7 belongs to class bromides-buliding-blocks, name is 5-Bromo-6-hydroxynicotinic acid, and the molecular formula is C6H4BrNO3, Computed Properties of 41668-13-7.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Henry, James R. published the artcileDiscovery of 1-(3,3-Dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a Pan-RAF Inhibitor with Minimal Paradoxical Activation and Activity against BRAF or RAS Mutant Tumor Cells, Name: 1-Bromo-4-fluoro-2-methylbenzene, the main research area is antitumor RAF inhibitor LY3009120 preparation structure activity cancer.

The RAS-RAF-MEK-MAPK cascade is an essential signaling pathway, with activation typically mediated through cell surface receptors. The kinase inhibitors vemurafenib and dabrafenib, which target oncogenic BRAF V600E, have shown significant clin. efficacy in melanoma patients harboring this mutation. Because of paradoxical pathway activation, both agents were demonstrated to promote growth and metastasis of tumor cells with RAS mutations in preclin. models and are contraindicated for treatment of cancer patients with BRAF WT background, including patients with KRAS or NRAS mutations. To eliminate the issues associated with paradoxical MAPK pathway activation and to provide therapeutic benefit to patients with RAS mutant cancers, we sought to identify a compound not only active against BRAF V600E but also wild type BRAF and CRAF. On the basis of its superior in vitro and in vivo profile, compound 13 was selected for further development and is currently being evaluated in phase I clin. studies.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 452-63-1 belongs to class bromides-buliding-blocks, name is 1-Bromo-4-fluoro-2-methylbenzene, and the molecular formula is C7H6BrF, Name: 1-Bromo-4-fluoro-2-methylbenzene.

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

Rice, Kenneth D. published the artcilePyrazolopyrimidines as dual Akt/p70S6K inhibitors, SDS of cas: 74896-66-5, the main research area is pyrazolopyrimidine preparation Akt p70S6K inhibitor SAR.

Activation of the PI3K/Akt/mTOR kinase pathway is frequently associated with human cancer. Selective inhibition of p70S6 Kinase, which is the last kinase in the PI3K pathway, is not sufficient for strong tumor growth inhibition and can lead to activation of upstream proteins including Akt through relief of a neg. feedback loop. Targeting multiple sites in the PI3K pathway might be beneficial for optimal activity. In this manuscript we report the design of dual Akt/p70S6K inhibitors and the evaluation of the lead compound 11b (I) in vivo, which was eventually advanced into clin. development.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 74896-66-5 belongs to class bromides-buliding-blocks, name is Methyl 3,5-dibromo-4-methylbenzoate, and the molecular formula is C9H8Br2O2, SDS of cas: 74896-66-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Aoyama, Hiroshi published the artcileFused heterocyclic amido compounds as anti-hepatitis C virus agents, Safety of 2-Bromo-4-methoxybenzoic acid, the main research area is fused heterocyclic amido compound preparation antiviral hepatitis C.

We identified a fused heteroaromatic amido structure based on the phenanthridine skeleton as a superior scaffold for candidate drugs with potent anti-HCV activity. Among the compounds synthesized, a phenanthridine analog with a 1,3-dioxolyl group (24) possessed the most potent anti-HCV activity (EC50 value: 50 nM), with acceptable cytotoxicity. The structural development and structure-activity relationships of these compounds are described.

Bioorganic & Medicinal Chemistry published new progress about Antiviral agents. 74317-85-4 belongs to class bromides-buliding-blocks, name is 2-Bromo-4-methoxybenzoic acid, and the molecular formula is C8H7BrO3, Safety of 2-Bromo-4-methoxybenzoic acid.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Yang, Fen-Fen published the artcileSynthesis and antibacterial activity studies in vitro of indirubin-3′-monoximes, COA of Formula: C8H7BrO3, the main research area is indirubin monoxime preparation antibacterial activity.

Multi-drug-resistant microbial pathogens are a serious global health problem. New compounds with antibacterial activity serve as good candidates for developing novel antibacterial drugs which is very urgent and important. In this work, based on the unique scaffold of indirubin, an active ingredient of traditional Chinese medicine formulation Danggui Luhui Wan, we synthesized 29 indirubin-3′-monoximes and preliminarily evaluated their antibacterial activities. The antibacterial activity results demonstrated that the synthesized indirubin-3′-monoximes 5a-5z and 5aa-5ad displayed good potency against S. aureus ATCC25923 (MIC = 0.4-25.6 μg mL-1). Among them, we found that the 5-F, 5-Cl and 7-CF3 substituted indirubin-3′;-monoximes 5r, 5s and 5aa also showed better antibacterial efficiency for S. aureus (MICs up to 0.4 μg mL-1) than the prototype natural product indirubin (MIC = 32 μg mL-1). More importantly, indirubin-3′-monoxime 5aa has certain synergistic effect with levofloxacin against clinic multidrug-resistant S. aureus (fractional inhibitory concentration index: 0.375). In addition, relevant experiments including electron microscopy observations, PI staining and the leakage of extracellular potassium ions and nucleic acid (260 nm) have been performed after treating S. aureus with indirubin-3′-monoxime 5aa, and the results revealed that indirubin-3′-monoximes could increase the cell membrane permeability of S. aureus. Although indirubin-3′-monoxime 5aa showed some cytotoxicity toward SH-SY5Y cells relative to compounds 5r and 5s, the skin irritation test of male mice after shaving showed that compound 5aa at a concentration of 12.8 μg mL-1 had no toxicity to mouse skin, and it could be used as a leading compound for skin antibacterial drugs.

RSC Advances published new progress about Antibacterial agents. 74317-85-4 belongs to class bromides-buliding-blocks, name is 2-Bromo-4-methoxybenzoic acid, and the molecular formula is C8H7BrO3, COA of Formula: C8H7BrO3.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Davey, Tim W. published the artcileSynthesis of ω-hydroxy quaternary ammonium bolaform surfactants, Related Products of bromides-buliding-blocks, the main research area is hydroxy quaternary ammonium bolaform surfactant synthesis.

Several members of a novel class of ω-substituted asym. bolaform surfactants were synthesized to investigate their surfactant and biol. properties. The ω-hydroxy trialkylammonium and pyridinium surfactants have significant antimicrobial and antifungal activity relative to their conventional analogs. For conventional quaternary ammonium alkyl surfactants, increasing the hydrocarbon chain length causes a decrease in the surfactant monomer solubility and a corresponding decrease in the biol. activity. No such trend is observed for the ω-hydroxy quaternary ammonium bromide series.

Australian Journal of Chemistry published new progress about Antimicrobial agents. 56523-59-2 belongs to class bromides-buliding-blocks, name is 15-Bromopentadecanoic acid, and the molecular formula is C15H29BrO2, Related Products of bromides-buliding-blocks.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Tuxen, Jens published the artcileHighly Fluorous Porphyrins as Model Compounds for Molecule Interferometry, Recommanded Product: Methyl 3,5-dibromo-4-methylbenzoate, the main research area is porphyrin perfluoroalkyl preparation quantum interference.

The synthesis and characterization of seven tailor-made highly fluorous porphyrin derivatives are described, as large perfluoroalkyl-functionalized organic mols. are the most complex objects for which the quantum wave nature has been observed so far. We have found, in particular, that tetrakis(pentafluorophenyl)porphyrin is a suitable starting point for a modular synthesis that is geared towards porphyrin derivatives with many peripheral fluorous chains. This allows us to tailor and optimize the sublimation features of these compounds for mol. interferometry. We have analyzed the evaporation process of one member of the series by determining the enthalpy of evaporation, as the creation of a sufficiently intense, slow mol. beam is crucial for quantum interference experiments We present the quantum fringe pattern of a second member of the series, which we could obtain in a Kapitza-Dirac-Talbot-Lau interferometer.

European Journal of Organic Chemistry published new progress about Evaporation enthalpy. 74896-66-5 belongs to class bromides-buliding-blocks, name is Methyl 3,5-dibromo-4-methylbenzoate, and the molecular formula is C9H8Br2O2, Recommanded Product: Methyl 3,5-dibromo-4-methylbenzoate.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary