Month: October 2022

Nakazato, Atsuro; Ohta, Kohmei; Sekiguchi, Yoshinori; Okuyama, Shigeru; Chaki, Shigeyuki; Kawashima, Yutaka; Hatayama, Katsuo published the artcile< Design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine σ ligands as potential antipsychotic drugs>, Category: chlorides-buliding-blocks, the main research area is arylalkoxyphenylalkylamine preparation sigma ligand antipsychotic; structure activity arylalkoxyphenylalkylamine antipsychotic; sigma receptor antagonist arylalkoxyphenylalkylamine.

σ-Receptor antagonists may be effective antipsychotic drugs that do not induce motor side effects caused by ingestion of classical drugs such as haloperidol. The authors obtained evidence that 1-(2-dipropylaminoethyl)-4-methoxy-6H-dibenzo[b,d]pyran hydrochloride (I) had selective affinity for σ receptor over dopamine D2 receptor. This compound was designed to eliminate two bonds of apomorphine (II) to produce structural flexibility for the nitrogen atom and to bridge two benzene rings with a -CH2O- bond to maintain the planar structure. In light of the evidence, N,N-dipropyl-2-(4-methoxy-3-benzyloxyphenyl)ethylamine (III) was designed. Since compound III had eliminated a biphenyl bond of 6H-dibenzo[b,d]pyran derivative I, it might be more released from the rigid structure of apomorphine II than compound I. The chem. modification of compound III led to the discovery that N,N-dipropyl-2- [4-methoxy-3-(2-phenylethoxy)phenyl]ethylamine hydrochloride (NE- 100), the best compound among arylalkoxyphenylalkylamine derivatives, had a high and selective affinity for σ receptor and had a potent activity in an animal model when the drug was given orally. The authors report here the design, synthesis, structure-activity relationships, and biol. characterization of novel arylalkoxyphenylalkylamine derivatives such as III.

Journal of Medicinal Chemistry published new progress about Antipsychotics. 22717-55-1 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO3, Category: chlorides-buliding-blocks.

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

Zhang, Yang-Ming; Gu, Min; Ma, Hui; Tang, Jie; Lu, Wei; Nan, Fa-Jun published the artcile< An efficient synthesis of 2-chloropyrimidines via Pd-catalyzed regioselective dechlorination of 2,4-dichloropyrimidines in the presence of NaHCO3>, Name: 2,6-Dichloro-9-methyl-9H-purine, the main research area is chloropyrimidine regioselective dechlorination palladium catalyst sodium hydrocarbonate; pyrimidine chloro preparation.

An efficient synthesis of 2-chloropyrimidines from readily accessible 2,4-dichloropyrimidines was achieved via Pd-catalyzed regioselective dechlorination in the presence NaHCO3.

Chinese Journal of Chemistry published new progress about Dechlorination (regioselective). 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Name: 2,6-Dichloro-9-methyl-9H-purine.

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

Wang, Chunyu; Liu, Yingze; Shao, Yue; Tang, Zian; Wen, Zhendong; Liang, Fuxin; Yang, Zhenzhong published the artcile< Zwitterionic Polymer Hairy Coating onto Mesh toward Easy Oil/Water Separation>, COA of Formula: C9H9Cl, the main research area is zwitterionic sulfobetaine methacrylate polymer graft coating stainless steel mesh; oil water separation membrane coating stainless steel mesh; coating; hairy structures; meshes; oil/water separation; zwitterionic polymers.

A zwitterionic polymeric hair-coated stainless steel mesh membrane is fabricated, which demonstrates efficient separation of oil/H2O mixtures and emulsions. The hairy coating of poly(divinylbenzene-co-vinylbenzene chloride) is generated by precipitation cationic polymerization, and subsequently grafting a zwitterionic polymer layer by atom transfer radical polymerization of sulfobetaine methacrylate. The microstructure of the hairy coating is tunable from an array of individual nanofibers to porous networks by interweaving of the hairs. The long-range attraction of zwitterionic polymers with H2O renders the coated mesh with excellent superhydrophilic and underwater superoleophobic performance. The coated mesh is highly antifouling to avoid the prehydration in conventional methods. Also, the microstructure is responsible for the high separation efficiency of oil/H2O emulsion. Therefore, separation of oil/H2O mixtures and emulsions becomes easier by the coated mesh, which is promising in industrial oil field sewage treatment.

Macromolecular Rapid Communications published new progress about Atom transfer radical polymerization. 1592-20-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H9Cl, COA of Formula: C9H9Cl.

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

Peng, Long; Li, Yuqiang; Li, Yangyang; Wang, Wang; Pang, Hailiang; Yin, Guoyin published the artcile< Ligand-Controlled Nickel-Catalyzed Reductive Relay Cross-Coupling of Alkyl Bromides and Aryl Bromides>, Recommanded Product: 3-Chlorophenethyl Bromide, the main research area is regioselective synthesis arylalkane; ligand controlled nickel catalyzed reductive relay cross coupling; alkyl bromide reductive relay cross coupling aryl bromide.

1,1-Diarylalkanes are important structural frameworks which are widespread in biol. active mols. Herein, we report a reductive relay cross-coupling of alkyl bromides with aryl bromides by nickel catalysis with a simple nitrogen-containing ligand. This method selectively affords 1,1-diarylalkane derivatives with good to excellent yields and regioselectivity.

ACS Catalysis published new progress about Alkylarenes Role: SPN (Synthetic Preparation), PREP (Preparation) (1,1-diarylalkanes). 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Recommanded Product: 3-Chlorophenethyl Bromide.

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

Zhou, Qingxin; Lin, Meihua; Feng, Xing; Ma, Fei; Zhu, Yuekun; Liu, Xing; Qu, Chao; Sui, Hong; Sun, Bei; Zhu, Anlong; Zhang, Heng; Huang, He; Gao, Zhi; Zhao, Yongxiang; Sun, Jiangyun; Bai, Yuxian; Jin, Junfei; Hong, Xuehui; Zou, Chang; Zhang, Zhiyong published the artcile< Targeting CLK3 inhibits the progression of cholangiocarcinoma by reprogramming nucleotide metabolism>, Related Products of 6055-19-2, the main research area is cholangiocarcinoma CLK3 serine threonine tyrosine nucleotide metabolism.

CDC-like kinase 3 (CLK3) is a dual specificity kinase that functions on substrates containing serine/threonine and tyrosine. But its role in human cancer remains unknown. Herein, we demonstrated that CLK3 was significantly up-regulated in cholangiocarcinoma (CCA) and identified a recurrent Q607R somatic substitution that represented a gain-of-function mutation in the CLK3 kinase domain. Gene ontol. term enrichment suggested that high CLK3 expression in CCA patients mainly was associated with nucleotide metabolism reprogramming, which was further confirmed by comparing metabolic profiling of CCA cells. CLK3 directly phosphorylated USP13 at Y708, which promoted its binding to c-Myc, thereby preventing Fbxl14-mediated c-Myc ubiquitination and activating the transcription of purine metabolic genes. Notably, the CCA-associated CLK3-Q607R mutant induced USP13-Y708 phosphorylation and enhanced the activity of c-Myc. In turn, c-Myc transcriptionally up-regulated CLK3. Finally, we identified tacrine hydrochloride as a potential drug to inhibit aberrant CLK3-induced CCA. These findings demonstrate that CLK3 plays a crucial role in CCA purine metabolism, suggesting a potential therapeutic utility.

Journal of Experimental Medicine published new progress about Cell infiltration. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Related Products of 6055-19-2.

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

Qin, Hongwei; Gao, Qingdong; Niu, Huiming; Wang, Zhefeng; Zhu, Xiaolin; Li, Jinlian; Yuan, Xing; Wu, Dongmei published the artcile< An in situ electrochemical detection method of cell viability>, Quality Control of 6055-19-2, the main research area is electrochem electrode cell viability culture.

An in situ electrochem. method of cell viability, which integrated cell culture, pretreatment and detection in a cell culture dish, was developed. The method significantly improved the electrochem. response of cells, simplified the operation process, reduced the experiment time, avoided the use of trypsin, and was applied in the study of the effectiveness of antitumor drugs on tumor suppression.

Analyst (Cambridge, United Kingdom) published new progress about Animal tissue culture. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Quality Control of 6055-19-2.

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

Jung, Hyun Joo; Chen, Zheng; Fayad, Luis; Wang, Michael; Romaguera, Jorge; Kwak, Larry W.; McCarty, Nami published the artcile< Bortezomib-resistant nuclear factor κB expression in stem-like cells in mantle cell lymphoma>, COA of Formula: C7H17Cl2N2O3P, the main research area is bortezomib resistance NFkappaB stem like mantle cell lymphoma.

Mantle cell lymphoma (MCL) is a subtype of B-cell Non-Hodgkin’s Lymphoma (NHL) and accounts for approx. 6% of all lymphomas. Unlike small lymphocytic lymphoma and chronic lymphocytic lymphoma, which are relatively sensitive to chemotherapy, MCL is highly refractory to most chemotherapy, and has the worst survival rate among NHL patients. Stem-like cells in MCL, which we have termed mantle cell lymphoma-initiating cells (MCL-ICs), enriched in the population that are lack of prototypic B-cell marker CD19. These cells were able to self-renew upon serial transplantation and are highly tumorigenic. Importantly, these stem-like cells confer chemotherapeutic resistance to MCL. In this report, we show that stem-like MCL-ICs are resistant to bortezomib, as well as chemotherapeutic regimens containing bortezomib, despite constitutive nuclear factor-κB (NF-κB) expression. Interestingly, bortezomib treatment induced MCL-IC differentiation in plasma-like cells with upregulated expression of CD38 and CD138. This process was accompanied by expression of plasma cell differentiation transcriptional factors, BLIMP-1 and IRF4. This article is the first to show that stem-like MCL cells utilize constitutive NF-κB expression for survival. Given that the NF-κB expression in MCL-ICs is resistant to bortezomib, it will be important to find alternative therapeutic strategies to inhibit NF-κB expression.

Experimental Hematology (New York, NY, United States) published new progress about Antitumor agent resistance. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, COA of Formula: C7H17Cl2N2O3P.

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

Manisha; Gupta, Shiv Shankar; Dhiman, Ankit Kumar; Sharma, Upendra published the artcile< Rh(III)-Catalyzed Selective C7 Halogenation of Indolines>, SDS of cas: 128-09-6, the main research area is haloindoline preparation regioselective halogenation halosuccinimide rhodium catalyst; pyrimidylindoline halosuccinimide halogenation rhodium catalyst regioselective.

An efficient Rh-catalyzed catalytic method has been developed for selective C7 halogenation of N-pyrimidyl indolines I (R = H, 5-Ph, 6-F, OCH2Ph, etc., R1 = H, 2-EtO2C, 3-Me, 2-Me, R2 = H) with N-halosuccinimides (halo = chloro, bromo, iodo) to produce the corresponding halides I (R2 = Br, Cl, I) in good to excellent yields. The advantages of this strategy include broad substrate scope and excellent regioselectivity for C7 functionalization of the indolines and feasibility at the gram scale level. Various control experiments have been performed to understand the reaction pathway. Applicability of current methodol. has been demonstrated by indole synthesis and post-transformation of the C7 halogenated indolines into different valuable mols. The reaction is also applicable to the preparation of halogenated carbazoles II (R2 = Br, Cl, I) and tetrahydroquinolines III (R2 = Br, I).

European Journal of Organic Chemistry published new progress about Carbazoles Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 128-09-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C4H4ClNO2, SDS of cas: 128-09-6.

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

Kolar, Michal; Hostas, Jiri; Hobza, Pavel published the artcile< The strength and directionality of a halogen bond are co-determined by the magnitude and size of the σ-hole>, Electric Literature of 1435-43-4, the main research area is halogen bond strength directionality sigma hole magnitude size effect.

The σ-holes of halogen atoms on various aromatic scaffolds were described in terms of their size and magnitude. The electrostatic potential maps at the CAM-B3LYP-D3(bj)/def2-QZVP level were calculated and the σ-holes of >100 aromatic analogs were thoroughly analyzed to relate the σ-holes to the binding preferences of the halogenated compounds Both the size and magnitude of the σ-hole increase when passing from chlorinated to iodinated analogs. Also, the σ-hole properties were studied upon chem. substitution of the aromatic ring as well as in the aromatic ring. Further, the angular variations of the interactions were studied on a selected set of halogenbenzene complexes with argon and hydrogen fluoride (HF). To analyze interaction energy components, DFT-SAPT angular scans were performed. The interaction energies of bromobenzene complexes were evaluated at the CCSD(T)/complete basis set level providing the benchmark energetic data. The strength of the halogen bond between halogenbenzenes and Ar atoms and HF mols. increases while its directionality decreases when passing from chlorine to iodine. The decrease of the directionality of the halogen bond is larger for a HF-containing complex and is caused by electrostatic and exchange-repulsion energies. These findings are especially valuable for protein-halogenated ligand-binding studies, applied in the realm of rational drug development and lead optimization.

Physical Chemistry Chemical Physics published new progress about Aryl halides Role: PRP (Properties). 1435-43-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H3ClF2, Electric Literature of 1435-43-4.

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

Han, Guang; Gu, Qinfen; Yang, Lei; Chen, Zhi-Gang; Zou, Jin published the artcile< A new indium selenide phase: controllable synthesis, phase transformation and photoluminescence properties>, Application of Cl3H8InO4, the main research area is indium selenide synthesis phase transformation photoluminescence.

A new indium selenide phase, close to the composition of In2.45Se4, is controllably synthesized by an EDTA-mediated solvothermal method. Through detailed structural and chem. characterization using transmission electron microscopy and synchrotron powder X-ray diffraction, it is determined that In2.45Se4 crystallizes in a rhombohedral structure with lattice parameters of a = 6.9632(1) Å and c = 38.1612(1) Å. Systematic investigations show that the synthesis parameters, including the reaction temperature, EDTA/InCl3 molar ratio, solvent composition, and reaction duration, play crucial roles in the formation of this new indium selenide phase. Naturally, such a new-phase In2.45Se4 easily forms flowerlike nano/micro-structures, while In2.45Se4 hexagonal nanoplates can also be selectively synthesized by tuning the precursor concentration In situ high-temperature synchrotron powder X-ray diffraction anal. demonstrates that In2.45Se4, with a hexagonal nanoplate morphol., is stable ≤400°, while a phase transformation from In2.45Se4 to γ-In2Se3 takes place when the annealing temperature reaches 500°. The photoluminescence property measurements show that the In2.45Se4 hexagonal nanoplates have a near IR emission at ∼815 nm, indicating their potential applications in optoelectronics.

Journal of Materials Chemistry C: Materials for Optical and Electronic Devices published new progress about Annealing. 22519-64-8 belongs to class chlorides-buliding-blocks, and the molecular formula is Cl3H8InO4, Application of Cl3H8InO4.

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