Month: October 2022

Kurppa, Kari J.; Liu, Yao; To, Ciric; Zhang, Tinghu; Fan, Mengyang; Vajdi, Amir; Knelson, Erik H.; Xie, Yingtian; Lim, Klothilda; Cejas, Paloma; Portell, Andrew; Lizotte, Patrick H.; Ficarro, Scott B.; Li, Shuai; Chen, Ting; Haikala, Heidi M.; Wang, Haiyun; Bahcall, Magda; Gao, Yang; Shalhout, Sophia; Boettcher, Steffen; Shin, Bo Hee; Thai, Tran; Wilkens, Margaret K.; Tillgren, Michelle L.; Mushajiang, Mierzhati; Xu, Man; Choi, Jihyun; Bertram, Arrien A.; Ebert, Benjamin L.; Beroukhim, Rameen; Bandopadhayay, Pratiti; Awad, Mark M.; Gokhale, Prafulla C.; Kirschmeier, Paul T.; Marto, Jarrod A.; Camargo, Fernando D.; Haq, Rizwan; Paweletz, Cloud P.; Wong, Kwok-Kin; Barbie, David A.; Long, Henry W.; Gray, Nathanael S.; Janne, Pasi A. published the artcile< Treatment-Induced Tumor Dormancy through YAP-Mediated Transcriptional Reprogramming of the Apoptotic Pathway>, Recommanded Product: 3-Bromobenzotrifluoride, the main research area is tumor dormancy YAP transcriptional reprogramming apoptotic pathway; YAP; dormancy; drug resistance; drug tolerance; epidermal growth factor receptor; lung cancer; senescence.

Eradicating tumor dormancy that develops following epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) treatment of EGFR-mutant non-small cell lung cancer, is an attractive therapeutic strategy but the mechanisms governing this process are poorly understood. Blockade of ERK1/2 reactivation following EGFR TKI treatment by combined EGFR/MEK inhibition uncovers cells that survive by entering a senescence-like dormant state characterized by high YAP/TEAD activity. YAP/TEAD engage the epithelial-to-mesenchymal transition transcription factor SLUG to directly repress pro-apoptotic BMF, limiting drug-induced apoptosis. Pharmacol. co-inhibition of YAP and TEAD, or genetic deletion of YAP1, all deplete dormant cells by enhancing EGFR/MEK inhibition-induced apoptosis. Enhancing the initial efficacy of targeted therapies could ultimately lead to prolonged treatment responses in cancer patients.

Cancer Cell published new progress about Aging, animal. 401-78-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3, Recommanded Product: 3-Bromobenzotrifluoride.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Sun, Wenhao; Xiang, Yonggang; Jiang, Zhihui; Wang, Shengyao; Yang, Nan; Jin, Shangbin; Sun, Linhao; Teng, Huailong; Chen, Hao published the artcile< Designed polymeric conjugation motivates tunable activation of molecular oxygen in heterogeneous organic photosynthesis>, Product Details of C7H8BrN, the main research area is thioether photocatalyst oxidation; sulfoxide preparation; aryl methanamine photocatalyst oxidative coupling reaction; diaryl azapropene preparation.

Herein, the first identification of tunable mol. oxygen activation induced by polymeric conjugation in nonmetallic conjugated microporous polymers (CMP) was reported. The conjugation between these can be achieved by the introduction of alkynyl groups. CMP-A with an alkynyl bridge facilitates the intramol. charge mobility while CMP-D, lacking an alkynyl group enhances the photoexcited carrier build-up on the surface from diffusion. These different processes dominate the directed ROS generation of the superoxide radical (·O-2) and singlet oxygen (1O2), resp. This theory is substantiated by the different performances of these CMPs in the aerobic oxidation of sulfides and the dehydrogenative coupling of amines, and could provide insight into the rational design of CMPs for various heterogeneous organic photosynthesis.

Science Bulletin published new progress about Aromatic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3959-07-7 belongs to class bromides-buliding-blocks, and the molecular formula is C7H8BrN, Product Details of C7H8BrN.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Parhi, Biswajit; Gurjar, Jitendra; Pramanik, Suman; Midya, Abhisek; Ghorai, Prasanta published the artcile< Organocatalytic Enantioselective Intramolecular Oxa-Michael Reaction of Enols: Synthesis of Chiral Isochromenes>, Computed Properties of 89003-95-2, the main research area is isochromene enantioselective synthesis; oxa Michael reaction enol squaramide catalyst.

An unprecedented enantioselective intramol. oxa-Michael reaction of enols has been described. A squaramide-containing tertiary amine based bifunctional organocatalyst efficiently activates the o-homoformyl chalcones to provide the chiral isochromenes in moderate yields and good to excellent enantioselectivities. Further, late-stage functionalizations of the vinyl ether moiety of the chiral isochromene products have also been exemplified.

Journal of Organic Chemistry published new progress about Benzopyrans Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 89003-95-2 belongs to class bromides-buliding-blocks, and the molecular formula is C8H4BrNO, Computed Properties of 89003-95-2.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Heinrich, Timo; Peterson, Carl; Schneider, Richard; Garg, Sakshi; Schwarz, Daniel; Gunera, Jakub; Seshire, Anita; Koetzner, Lisa; Schlesiger, Sarah; Musil, Djordje; Schilke, Heike; Doerfel, Benjamin; Diehl, Patrizia; Boepple, Pia; Lemos, Ana R.; Sousa, Pedro M. F.; Freire, Filipe; Bandeiras, Tiago M.; Carswell, Emma; Pearson, Nicholas; Sirohi, Sameer; Hooker, Mollie; Trivier, Elisabeth; Broome, Rebecca; Balsiger, Alexander; Crowden, Abigail; Dillon, Christian; Wienke, Dirk published the artcile< Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106>, Recommanded Product: 3-Bromobenzotrifluoride, the main research area is pyrazoloindole carboxylic TEAD binding fragment hit lead.

The dysregulated Hippo pathway and, consequently, hyperactivity of the transcriptional YAP/TAZ-TEAD complexes is associated with diseases such as cancer. Prevention of YAP/TAZ-TEAD triggered gene transcription is an attractive strategy for therapeutic intervention. The deeply buried and conserved lipidation pocket (P-site) of the TEAD transcription factors is druggable. The discovery and optimization of a P-site binding fragment are described. Utilizing structure-based design, enhancement in target potency was engineered into the hit, capitalizing on the established X-ray structure of TEAD1. The efforts culminated in the optimized in vivo tool MSC-4106 (I), which exhibited desirable potency, mouse pharmacokinetic properties, and in vivo efficacy. In close correlation to compound exposure, the time- and dose-dependent downregulation of a proximal biomarker could be shown.

Journal of Medicinal Chemistry published new progress about Fused heterocyclic compounds Role: PAC (Pharmacological Activity), PKT (Pharmacokinetics), PRP (Properties), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses). 401-78-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3, Recommanded Product: 3-Bromobenzotrifluoride.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Huang, Jin; Fu, Ronghui; Jing, Linhai; Qin, Dabin; Huang, Kun; Wang, Wei published the artcile< A convenient access to 3-substituted benzofuran derivatives via palladium nanoparticles-catalyzed intramolecular Heck reaction>, Recommanded Product: 2-Bromo-4-(trifluoromethyl)phenol, the main research area is benzofuran palladium nanoparticle catalyst intramol Heck reaction.

A concise and efficiently route for the synthesis of 3-substituted benzofurans via the intramol. Heck reaction of bromoaryl 3-phenylallyl ethers has been developed. This simple and highly efficient palladium nanoparticles-catalyzed system showed good catalytic activity. The desired products were afforded in good to high yields (45%∼96%).

Youji Huaxue published new progress about Heck reaction. 81107-97-3 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3O, Recommanded Product: 2-Bromo-4-(trifluoromethyl)phenol.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zheng, Yuanqin; Zhou, Yuqiao; Zhang, Yan; Deng, Pengchi; Zhao, Xiaohu; Jiang, Shichao; Du, Guangxi; Shen, Xin; Xie, Xinyu; Su, Zhishan; Yu, Zhipeng published the artcile< Water-Involved Ring-Opening of 4-Phenyl-1,2,4-triazoline-3,5-dione for ""Photo-Clicked"" Access to Carbamoyl Formazan Photoswitches In Situ>, Computed Properties of 401-78-5, the main research area is functionalized carbamoyl formazan photochem preparation DFT NBO; diarylsydnone phenyl triazolidine dione photoswitchable ring opening water promoted; Azo compounds; Diarylsydnones; Photo-ligation; Photoswitches; Umpolung.

A “”photo-click”” method that involved nitrile imine from diarylsydnone to capture diazenecarbonyl-phenyl-carbamic acid (DACPA) generated by water-promoted ring-opening of PTAD was described. DFT calculation revealed that H-bonding interactions between PTAD and water were vital to form DACPA which exhibited an umpolung effect during ligation by nature bond orbit anal. (NBO). The ultra-fast ligation resulted in carbamoyl formazans, as a unique Z <-> E photo-switchable linker on target mols., including peptide and drugs, with excellent anti-fatigue performance. This strategy was showcased to construct highly functionalized carbamoyl formazans such as I [R = H, 4-F, 4-Ph, etc.; R1 = 4-CF3, 3-CN, etc.; R2 = H, 4-F, 4-MeO, etc.] in situ for photo-pharmacol. and material studies, which also expanded chem. of PTAD in aqueous media.

Chemistry – An Asian Journal published new progress about Decarboxylation. 401-78-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3, Computed Properties of 401-78-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Pump, Eva; Poater, Albert; Zirngast, Michaela; Torvisco, Ana; Fischer, Roland; Cavallo, Luigi; Slugovc, Christian published the artcile< Impact of Electronic Modification of the Chelating Benzylidene Ligand in cis-Dichloro-Configured Second-Generation Olefin Metathesis Catalysts on Their Activity>, SDS of cas: 16426-64-5, the main research area is benzylidene ruthenium imidazolidene carbene chelating complex preparation catalyst polymerization; impact electronic modification chelating benzylidene ruthenium dichloro metathesis catalyst; configured olefin metathesis catalyst benzylidene ruthenium imidazolidene carbene complex; cis trans isomerization benzylidene ruthenium imidazolidene carbene dichloro complex; crystal mol structure benzylidene ruthenium imidazolidene carbene chelating complex.

A series of electronically modified second-generation cis-dichloro ruthenium ester chelating benzylidene complexes was prepared, characterized, and benchmarked in a typical ring-opening metathesis polymerization (ROMP) experiment The electronic tuning of the parent chelating benzylidene ligand (2-Et ester benzylidene) was achieved by substitution at the 4- and 5-positions with electron-withdrawing nitro or electron-donating methoxy groups. The effect of the electronic tuning on the cis-trans isomerization process was studied exptl. and theor. D. functional theory calculations clearly revealed the influence of electronic modification on the relative stability between the cis and trans isomers, which is decisive for the activity of the studied compounds as initiators in ROMP.

Organometallics published new progress about Alkenes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, SDS of cas: 16426-64-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Wang, Shengzheng; Chen, Shuqiang; Guo, Zhongjie; He, Shipeng; Zhang, Fan; Liu, Xueying; Chen, Weiping; Zhang, Shengyong; Sheng, Chunquan published the artcile< Synthesis of spiro-tetrahydrothiopyran-oxindoles by Michael-aldol cascade reactions: discovery of potential P53-MDM2 inhibitors with good antitumor activity>, Related Products of 3893-18-3, the main research area is spiro tetrahydrothiopyran oxindole diastereoselective preparation SAR antitumor; indolinone unsaturated aldehyde Michael aldol cascade proline catalyst.

Using proline as a catalyst, an organocatalytic Michael-aldol cascade reaction was developed for the synthesis of spiro-tetrahydrothiopyran oxindoles I [R1 = H, F, Me, Cl, Br; R2 = 2-furyl, Ph, 4-BrC6H4, etc.; R3 = Et, n-Pr, Ph, etc.] from indolinones and α,β-unsaturated aldehydes. The highly functionalized scaffold was assembled in moderate to good yields (51-78%) and excellent diastereoselectivities (>20 : 1 dr). Interestingly, the oxindoles I displayed moderate to good in vitro antitumor activities and were validated as p53-MDM2 inhibitors, which represented promising lead compounds for antitumor drug discovery.

Organic & Biomolecular Chemistry published new progress about Aldol condensation catalysts, stereoselective. 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Related Products of 3893-18-3.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Xie, Hui; Hu, Wanshan; Zhang, Fei; Zhao, Changbo; Peng, Tingting; Zhu, Caizhen; Xu, Jian published the artcile< AIE-active polyelectrolyte based photosensitizers: the effects of structure on antibiotic-resistant bacterial sensing and killing and pollutant decomposition>, Safety of 1,2-Bis(4-bromophenyl)-1,2-diphenylethene, the main research area is antibiotic resistant bacterial sensing killing pollutant decomposition photosensitizer; aggregation induced emission polyelectrolyte.

A facile and effective multifunctional platform with high bacterial detection sensitivity, good antibacterial activity, and excellent dye decomposition efficiency holds great promise for wastewater treatment. To explore the design rationality and mechanism of material platforms with various integrated components into a single mol. for wastewater treatment applications, herein, four kinds of polyelectrolyte photosensitizers with aggregation-induced emission (AIE) fluorescent units are synthesized and systematically studied to investigate the structure-property relationship that influences the level of conjugation and the hydrophobicity-hydrophilicity balance. By improving the strength of the conjugation, the new AIE photosensitizers DBPVEs (including DBPVE-4 and DBPVE-6) generate a reactive oxygen species (ROS), and a decomposition efficiency of around 55% is obtained for dyes when they are exposed to DBPVEs under white light irradiation, which is higher than those of DBPEs (including DBPE-4 and DBPE-6). More importantly, owing to the longer and more flexible aliphatic chains of DBPVE-6 that facilitate efficient intercalation into cell membranes, the staining ability of DBPVE-6 for methicillin-resistant S. epidermidis (MRSE) is greatly enhanced as compared to that of DBPVE-4. It should be noted that the antibacterial experiment indicates that DBPVE-6 displays potent toxicity to MRSE with 99.9% killing efficiency under white light irradiation This work provides essential theor. and exptl. guidance on the designing of new photosensitizers for wastewater treatment.

Journal of Materials Chemistry B: Materials for Biology and Medicine published new progress about Aggregation-induced emission. 184239-35-8 belongs to class bromides-buliding-blocks, and the molecular formula is C26H18Br2, Safety of 1,2-Bis(4-bromophenyl)-1,2-diphenylethene.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Yanai, Hikaru; Egawa, Saki; Yamada, Kenta; Ono, Junpei; Aoki, Motohide; Matsumoto, Takashi; Taguchi, Takeo published the artcile< 1,1-Bis(triflyl)alkadienes: Easy-To-Handle Building Blocks for Strongly Acidic Carbon Acids>, Synthetic Route of 3893-18-3, the main research area is unsaturated aldehyde triflylmethane condensation; bistriflylalkadiene preparation Mukaiyama aldol; carbon acid preparation catalysis.

1,1-Bis(triflyl)alkadienes I (Ar = C6H5, 4-CH3C6H4, 4-CH3OC6H4, 3-EtOC6H4, 4-ClC6H4, 2-BrC6H4, etc.) were easily prepared by mixing bis(triflyl)methane and α,β-unsaturated aldehydes and then used as easy-to-handle building blocks for the preparation of strongly acidic carbon acids. The reaction of these alkadienes with either NaBH4 or organocerium reagents gave the desired carbon acids through a β-selective nucleophilic addition reaction. Similar reactions of a 1,1-bis(trifyl)alkadiene with sterically bulky iPrMgBr resulted in a δ-selective alkylation instead. The present β-alkylation is the realization of the synthesis of β-branched 1,1-bis(triflyl)alkanes with an acidic C-H moiety. Furthermore, when submitted to a Mukaiyama aldol reaction, β-branched carbon acids had a higher catalyst activity than that of the corresponding nonbranched carbon acids.

Asian Journal of Organic Chemistry published new progress about Acidity. 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Synthetic Route of 3893-18-3.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary