Month: November 2022

On August 31, 2020, Miura, Kazuki; Onodera, Chihiro; Takagi, Motonari; Koyama, Ryosuke; Hirano, Takako; Nishio, Toshiyuki; Hakamata, Wataru published an article.Recommanded Product: 2567-29-5 The title of the article was Screening, synthesis, and evaluation of novel isoflavone derivatives as inhibitors of human Golgi β-galactosidase. And the article contained the following:

The genes GLB1 and GALC encode GLB1 isoform 1 and galactocerebrosidase, resp., which exhibit β-galactosidase activity in human lysosomes. GLB1 isoform 1 has been reported to play roles in rare lysosomal storage diseases. In this study, we first constructed a cell-based high-throughput screening (HTS) system for Golgi β-galactosidase inhibitors, and then screened inhibitors from two compound libraries using the HTS system, in vitro assay, and cytotoxicity assay. An isoflavone derivative was identified among the final Golgi β-galactosidase inhibitor compound hits. Mol. docking simulations were performed to redesign the isoflavone derivative into a more potent inhibitor, and six designed derivatives were then synthesized. One of the derivatives, ARM07, exhibited potent inhibitory activity against β-galactosidase, with an IC50 value of 14.8 μM and competitive inhibition with Ki value of 13.3 μM. Furthermore, the in vitro and cellular inhibitory activities of ARM07 exceeded those of deoxygalactonojirimycin. ARM07 may contribute to the development of affinity-based chem. probes to identify the protein responsible for the newly discovered Golgi β-galactosidase activity. The therapeutic relevance of ARM07 against lysosomal storage diseases and its effect on senescent cells should be evaluated further. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Recommanded Product: 2567-29-5

The Article related to krabbe disease glb1 galactocerebrosidase mol docking simulation, inhibitor screening, isoflavone, lysosomal storage disease, senescence-associated β-galactosidase, β-galactosidase and other aspects.Recommanded Product: 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On June 11, 2020, Sunwoo, Kyoung; Won, Miae; Ko, Kyung-Phil; Choi, Miri; Arambula, Jonathan F.; Chi, Sung-Gil; Sessler, Jonathan L.; Verwilst, Peter; Kim, Jong Seung published an article.Electric Literature of 83152-22-1 The title of the article was Mitochondrial Relocation of a Common Synthetic Antibiotic: A Non-genotoxic Approach to Cancer Therapy. And the article contained the following:

Tumor recurrence as a result of therapy-induced nuclear DNA lesions is a major issue in cancer treatment. Currently, only a few examples of potentially non-genotoxic drugs have been reported. Mitochondrial re-localization of ciprofloxacin, one of the most commonly prescribed synthetic antibiotics, is reported here as a new approach. Conjugation of ciprofloxacin to a tri-Ph phosphonium group (giving lead Mt-CFX) is used to enhance the concentration of ciprofloxacin in the mitochondria of cancer cells. The localization of Mt-CFX to the mitochondria induces oxidative damage to proteins, mtDNA, and lipids. A large bias in favor of mtDNA damage over nDNA was seen with Mt-CFX, contrary to classic cancer chemotherapeutics. Mt-CFX was found to reduce cancer growth in a xenograft mouse model and proved to be well tolerated. Mitochondrial re-localization of antibiotics could emerge as a useful approach to generating anticancer leads that promote cell death via the selective induction of mitochondrially mediated oxidative damage. The experimental process involved the reaction of (6-Bromohexyl)triphenylphosphonium bromide(cas: 83152-22-1).Electric Literature of 83152-22-1

The Article related to breast cancer cell death mitochondria ciprofloxacin, ciprofloxacin, dna damage, mitochondria, non-genotoxic cancer therapy, prodrug, reactive oxygen species, targeted therapeutics and other aspects.Electric Literature of 83152-22-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On October 7, 2015, Myung, Beom Yeong; Yoon, Tae Ho published a patent.Application of 41819-13-0 The title of the patent was Method for the preparation of fluorinated pyromellitic dianhydride. And the patent contained the following:

Disclosed is a preparation method of I, characterized by (1) bromination of pyromellitic dianhydride to obtain II (2) successive reaction of Q1-Br with magnesium and trimethylborate followed by hydrolysis to obtain Q1-B(OH)2 (3) treatment of II with Q1-B(OH)2 in the presence of a catalyst (4) sublimation of the resulting compound III under reduced pressure [R1, R2 = independently H or Q1; with a proviso that R1 and R2 cannot be H simultaneously; R3, R4 = independently fluorinated alkyl; A1, A2 = independently H or Br]. For example, bromination of pyromellitic dianhydride [dissolving in 33% aqueous NaOH → Br2 (addition over a period of 1 h), 90%], coupling reaction with 3,5-bis(trifluoromethyl)phenylboronic acid (preparation given) [Pd(PPh3)4, 2 N Na2CO3, toluene, 98°, 48 h, 72%] and cyclocondensation [drying (250°, 30 inHg vacuum pressure, 12 h) → sublimation (290°, 30 inHg vacuum pressure)] afforded compound I [R1 = R2 = 3,5-bis(trifluoromethyl)phenyl] (70% yield). Compound I is useful for the production of polyimide having low permittivity and high heat-resistance. The experimental process involved the reaction of 3,6-Dibromobenzene-1,2,4,5-tetracarboxylic acid(cas: 41819-13-0).Application of 41819-13-0

The Article related to fluoroalkylphenyl pyromellitic dianhydride preparation polyimide intermediate, grignard reaction borylation hydrolysis, bromination coupling reaction cyclocondensation sublimation and other aspects.Application of 41819-13-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On April 1, 2020, Wang, Guowei; Zhu, Dingcheng; Zhou, Zhuxian; Piao, Ying; Tang, Jianbin; Shen, Youqing published an article.COA of Formula: C13H11Br The title of the article was Glutathione-Specific and Intracellularly Labile Polymeric Nanocarrier for Efficient and Safe Cancer Gene Delivery. And the article contained the following:

Cationic polymers condense nucleic acids into nanosized complexes (polyplexes) that are widely explored for nonviral gene delivery, but their strong electrostatic binding with DNA causes inefficient intracellular gene release and translation and thereby unsatisfactory gene transfection efficiencies. Facilitated intracellular dissociation of polyplexes by making the polymer undergo pos.-to-neg./neutral charge reversal can effectively solve these problems, but they must be sufficiently stable during the delivery. Herein, we report the first glutathione (GSH)-specific intracellular labile polyplexes for cancer-targeted gene delivery. The polymers are made from p-(2,4-dinitrophenyloxybenzyl)-ammonium cationic moieties, whose p-2,4-dinitrophenyl ether is cleaved specifically by GSH, rather than other biol. thiols, triggering the conversion of the ammonium cation into the carboxylate anion and thus the fast intracellular DNA release of the polyplexes. Furthermore, the polyplexes coated with PEG-functionalized lipids are stable in biol. fluids to gain long blood circulation for tumor accumulation. Thus, the efficient tumor accumulation and cell transfection of the polyplexes loaded with the tumor suicide gene tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) give rise to potent antitumor activity similar to that of the first-line chemotherapy drug paclitaxel but with much less adverse effects. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).COA of Formula: C13H11Br

The Article related to tumor antitumor trail gene therapy vector glutathione, cancer gene delivery, charge-reversal polymer, gene release, glutathione-responsive polymer, nonviral vectors, polymeric vector and other aspects.COA of Formula: C13H11Br

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On October 14, 2021, Reynolds, Dominic; Leger, Serge; Seiler, Michael W.; Agrawal, Anant A.; Vaillancourt, Frederic; Smith, Peter; Hopper, Allen T.; Prajapati, Sudeep; Soueidan, Olivier published a patent.SDS of cas: 1196157-51-3 The title of the patent was Preparation of quinazolinone, phthalazinone and isoquinolinone compounds for modulating splicing. And the patent contained the following:

The present disclosure features compounds I [A = (un)substituted cycloalkyl, heterocyclyl, aryl, or heteroaryl; Rb = B, (un)substituted alkyl, or heteroalkyl; B = (un)substituted cycloalkyl, heterocyclyl, aryl, or heteroaryl; Y = N, (un)substituted CH, or CH2; R2 = (independently) H or alkyl; R3 = (halo)alkyl, halo, cyano, etc.; each of L1 and L2 = (independently) absent, alkylene, heteroalkylene, O, etc.; m = 0-3; n = 0-2] or pharmaceutically acceptable salts, and related compositions that, inter alia, modulate nucleic acid splicing, e.g., splicing of a pre-mRNA, as well as methods of use thereof. E.g., a multi-steps synthesis of II, starting from 2-methyl-2H-indazole-5-carboxylic acid, was described. Exemplified compounds I were tested for their RNA splicing modulatory activity (data given for representative compounds I). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of 2-Amino-6-bromonicotinic acid(cas: 1196157-51-3).SDS of cas: 1196157-51-3

The Article related to quinazolinone phthalazinone isoquinolinone preparation splicing nucleic acid rna modulator, premrna dna rna spliceosome modulator quinazolinone phthalazinone isoquinolinone preparation and other aspects.SDS of cas: 1196157-51-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On November 17, 2021, Bonnefoy, Clemence; Chefdeville, Emmanuel; Panosian, Armen; Hanquet, Gilles; Leroux, Frederic R.; Toulgoat, Fabien; Billard, Thierry published an article.Synthetic Route of 2567-29-5 The title of the article was Study of a Stable “Trifluoromethoxide Anion Solution” Arising from 2,4-Dinitro-Trifluoromethoxybenzene. And the article contained the following:

Despite recent advances, trifluoromethoxylation remains a challenging reaction. Here we describe an efficient trifluoromethoxylative substitution, using an inexpensive and easy-to-handle reagent. By mixing DMAP with a slight excess of 2,4-dinitro-trifluoromethoxybenzene (DNTFB), a stable solution of trifluoromethoxide anion is obtained and can be used to perform a SN2 reaction without any silver additives. A precise study of the properties and behavior of this unusual stable solution of CF3O- species is also performed. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Synthetic Route of 2567-29-5

The Article related to fluoromethoxylative substitution nitrotrifluoromethoxybenzene, 2,4-dinitro-trifluoromethoxybenzene, fluorine, nucleophilic substitution, trifluoromethoxide anion, trifluoromethoxylation and other aspects.Synthetic Route of 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On May 21, 2021, Weis, Erik; Hayes, Martin A.; Johansson, Magnus J.; Martin-Matute, Belen published an article.Application of 1427433-22-4 The title of the article was Iridium-catalyzed C-H methylation and d3-methylation of benzoic acids with application to late-stage functionalizations. And the article contained the following:

An iridium-catalyzed carboxylate-directed ortho C-H methylation and d3-methylation of benzoic acids was reported. The method used com. available reagents and precatalyst and requires no inert atm. or exclusion of moisture. Substrates bearing electron-rich and electron-poor groups were successfully methylated, including compounds with competing directing/coordinating groups. The method was also applied to the LSF of several marketed drugs, forming analogs with increased metabolic stability compared with the parent drug. The experimental process involved the reaction of 3-Bromo-2-fluoro-6-methyl-benzoic acid(cas: 1427433-22-4).Application of 1427433-22-4

The Article related to benzoic acid potassium methyltrifluoroborate iridium catalyst regioselective methylation, methylbenzoic acid preparation, applied chemistry, chemistry, green chemistry, organic chemistry and other aspects.Application of 1427433-22-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On February 28, 2022, Li, Zhi-Ying; Xu, Guang-Sen; Song, Yu-Liang; Li, Xun published an article.Application of 574-98-1 The title of the article was Structural optimizations and bioevaluation of N-substituted acridone derivatives as strong topoisomerase II inhibitors. And the article contained the following:

Previously, an array of N-substituted acridone derivatives have been reported as potent topoisomerase II (topo II) inhibitors, and preliminary structure-activity relationship (SAR) outcomes revealed that the linker between 1-NH and N-Me piperazine motif of the tricyclic acridone scaffold significantly affected their anti-proliferative potencies. To further explore the SARs of acridone-derived topo II inhibitors, a wider range of novel acridone derivatives were herein synthesized via two rounds of structural optimizations on two validated hits, E17 and E24. Initially, the linker length was optimized, and then influences of N-Me piperazinyl moiety and disposition of three N atoms on the bioactivity were investigated. As a result, a newly developed topo II inhibitor 6 h was found to be more potent than E17 and E24, thereby serving as a tool compound for the follow-up mechanistic study. Compound 6 h functioned as a strong topo IIα/β inhibitor, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential (Δψm). Further mol. docking and MD study illustrated the favorable interactions of 6 h with both topo IIα and topo IIβ subtypes. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Application of 574-98-1

The Article related to topoisomerase ii inhibitors structure activity relationship anticancer, n-substituted acridone derivatives, structural optimization, structure-activity relationship, topo iiα/β inhibitor and other aspects.Application of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On February 24, 2011, Sone, Toshihiko; Nakajima, Tomoko; Takai, Kentaro published a patent.Formula: C7H8BrCl2N The title of the patent was Preparation of bicyclic urea derivatives as soluble epoxide hydrolase inhibitors. And the patent contained the following:

Title compounds I [R1 = (un)substituted cycloalkyl, (un)substituted heterocyclyl, (un)substituted aryl, etc.; R2a, R2b = H, halo, hydroxy, etc.; m = 0-5; ring A = Q1, etc.; R3a, R3b, R3c = H, halo, hydroxy, etc.] or pharmaceutically acceptable salts thereof were prepared For example, alkxoycarbonylation of nortropine·HCl with Boc2O, reaction with 2-fluoropyridine, deprotection using HCl, and treatment with 4-(trifluoromethyl)phenylisocyanate afforded endo-II. In soluble epoxide hydrolase (sEH) inhibition assay, endo-II showed 97% inhibition activity. Compounds I are claimed useful for the treatment of hypertension, kidney disease (primary and secondary), etc. The experimental process involved the reaction of (4-Bromo-2-chlorophenyl)methanamine hydrochloride(cas: 874482-96-9).Formula: C7H8BrCl2N

The Article related to bicyclic urea preparation soluble epoxide hydrolase inhibitor, hypertension treatment bicyclic urea seh inhibition, primary secondary kidney disease treatment bicyclic urea seh inhibition and other aspects.Formula: C7H8BrCl2N

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Czopek, Anna; Partyka, Anna; Bucki, Adam; Pawlowski, Maciej; Kolaczkowski, Marcin; Siwek, Agata; Gluch-Lutwin, Monika; Koczurkiewicz, Paulina; Pekala, Ezzbieta; Jaromin, Anna; Tyliszczak, Bozena; Wesolowska, Anna; Zagorska, Agnieszka published an article in 2020, the title of the article was Impact of N-alkylamino substituents on serotonin receptor (5-HTR) affinity and phosphodiesterase 10A (PDE10A) inhibition of isoindole-1,3-dione derivatives.SDS of cas: 574-98-1 And the article contains the following content:

In this study, a series of compounds derived from 1H-isoindole-1,3(2H)-dione I (R = H, OMe; R1 = 1,2,3,4-tetrahydroisoquinolin-2-yl, 1,2,3,4-tetrahydroisoquinolin-2-yl, pyridin-2-yl, 1H-1,3-benzimidazol-2-yl, etc.; X = (CH2)n, n = 1-5), potential ligands of phosphodiesterase 10A and serotonin receptors, were investigated as potential antipsychotics. A library of I with various amine moieties was synthesized and examined for their phosphodiesterase 10A (PDE10A)-inhibiting properties and their 5-HT1A and 5-HT7 receptor affinities. Based on in vitro studies, the most potent compound, I [R = OMe; R1 = 1H-1,3-benzimidazol-2-yl; n = 4 (II)], was selected and its safety in vitro was evaluated. In order to explain the binding mode of compound II in the active site of the PDE10A enzyme and describe the mol. interactions responsible for its inhibition, computer-aided docking studies were performed. The potential antipsychotic properties of compound II in a behavioral model of schizophrenia were also investigated. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).SDS of cas: 574-98-1

The Article related to isoindoledione preparation phosphodiesterase inhibition serotonin receptor affinity antitumor activity, antipsychotic activity, benzimidazole derivatives, phosphodiesterase 10a, schizophrenia and other aspects.SDS of cas: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary