Category: 22483-09-6

Cho, Er-Chieh published the artcileRing size changes in the development of class I HDAC inhibitors, Category: alcohols-buliding-blocks, the main research area is thienylbenzamide anticancer SAR HDAC inhibitor docking; HDAC; Thienylbenzamides; colon cancer; ring transformation.

Five pathways involving different ring structures led to generation of fourteen thienylbenzamides which display the structure-activity relationships of class I HDAC inhibitors. All the synthesized compounds inhibit HDAC1 and HDAC2 selectively over other isoforms and many inhibit DLD1 and HCT116 cells more effectively than a parent compound Compounds and inhibit HCT116 cells by activation of the apoptosis pathway.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Antitumor agents. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Category: alcohols-buliding-blocks.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Song, Zilan published the artcileStructure-Activity Relationship Study of Amidobenzimidazole Analogues Leading to Potent and Systemically Administrable Stimulator of Interferon Gene (STING) Agonists, Application of 2,2-Dimethoxyethanamine, the main research area is amidobenzimidazole analog STING agonist SAR immunooncol.

Activation of the stimulator of interferon gene (STING) has emerged as an exciting immuno-oncol. therapeutic strategy; however, the first-generation STING agonists, cyclic dinucleotide (CDN) analogs, have suffered from many disadvantages and failed in clin. trials. Therefore, non-CDN small-mol. STING agonists are urgently needed. In view of the unique structure of the high potency of dimeric amidobenzimidazole STING agonist 5, a structural elaboration was conducted by modifying several structural hotspots of this scaffold. Triazole 40 was identified as a new potent STING activator, possessing EC50 values of 0.24 and 39.51μM for h- and m-STING, resp. This compound has a slightly better pharmacokinetic profile and is >20-fold more aqueously soluble than 5. It activated the STING signaling dramatically by directly binding and stabilizing all h-STING isoforms and m-STING. In vivo, intermittent administration of 40 (I) was found to have significant antitumor efficacy with good tolerance in two mouse tumor models.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Application of 2,2-Dimethoxyethanamine.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Gazizov, Almir S. published the artcileThe Highly Regioselective Synthesis of Novel Imidazolidin-2-ones via the Intramolecular Cyclization/Electrophilic Substitution of Urea Derivatives and the Evaluation of Their Anticancer Activity, Application In Synthesis of 22483-09-6, the main research area is imidazolidinone regioselective preparation anticancer human cytotoxicity quantum chem calculation; urea aromatic nucleophile intramol cyclization electrophilic substitution TFA catalyst; anti-cancer activity; anti-tumor activity; cyclization; cytotoxicity; imidazolidine-2-one; regioselectivity; urea.

A series of novel 4-(het)arylimidazolidin-2-ones I [R = 5-Cl-2,4-di-HO-C6H2, 6-hydroxy-1,3-benzodioxol-5-yl, 4-hydroxy-6-methyl-2-oxo-pyran-3-yl; R1 = H, Me; R2 = Ph, 4-MeC6H4, 3-ClC6H4, etc.] was obtained by the acid-catalyzed reaction of (2,2-dimethoxyethyl)ureas with aromatic and heterocyclic C-nucleophiles. The proposed approach to substituted imidazolidinones I benefited from excellent regioselectivity, readily available starting materials and a simple procedure. The regioselectivity of the reaction was rationalized by quantum chem. calculations and control experiments The anti-cancer activity of the obtained compounds was tested in vitro.

Molecules published new progress about Antitumor agents. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Application In Synthesis of 22483-09-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Qian, Yuyi published the artcileHighly Tumor-Specific and Long-Acting Iodine-131 Microbeads for Enhanced Treatment of Hepatocellular Carcinoma with Low-Dose Radio-Chemoembolization, Synthetic Route of 22483-09-6, the main research area is iodine 131 microbead transarterial radioembolization liver carcinoma; doxorubicin; hepatocellular carcinoma; iodine-131; transarterial radioembolization; tumor retention.

Transarterial radioembolization (TARE) is considered the standard treatment for intermediate-stage hepatocellular carcinoma (HCC). Iodine-131 (131I)-labeled lipiodol TARE is an effective treatment for HCC but has been withdrawn due to its poor retention in tumor lesions and significant distribution in normal tissues with severe side effects. In this work, a highly tumor-specific 131I-TARE agent with long-time retention is developed by simply introducing tyrosine to poly(vinyl alc.) (PVA) drug-eluting microbeads (Tyr-PVA-DEBs). The labeling efficiency of 131I-labeled microbeads remains above 85% in 50% serum for 31 days. Micro-single-photon emission computed tomog./computed tomog. (μSPECT/CT) evidences that the 131I-labeled microbeads accumulate in the orthotopic N1S1 hepatoma of rats for 31 days following intra-arterial injection. The cumulative radiation dose per cubic centimeter of the tumor is at least 13 678-fold higher than that of normal tissues. The highly tumor-selective radiation of the 131I-labeled microbeads allows localized delivery of 345.04 ± 139.16 Gy to the tumor following a single injection dose as low as 0.2 mCi of 131I. Moreover, the 131I-labeled microbeads are loaded with doxorubicin hydrochloride (DOX) through the carboxy groups on tyrosine of the polymer. The 131I-DOX-loaded microbeads present a synergetic antitumor effect without recurrence in comparison with the microbeads labeled with 131I or loading DOX alone, attributed to the sensitization of DOX to 131I-induced ionizing radiation damage to DNA under the embolization-induced hypoxia. Our results demonstrate a high tumor retention of 131I-labeled embolic agent for low-dose transarterial radio-chemoembolization (TARCE) with a synergetic therapeutic effect on treating HCC, showing potential for clin. application.

ACS Nano published new progress about Antitumor agents. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Synthetic Route of 22483-09-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Takemoto, Hiroyasu published the artcilePolymeric modification of gemcitabine via cyclic acetal linkage for enhanced anticancer potency with negligible side effects, SDS of cas: 22483-09-6, the main research area is anticancer drug gemcitabine polymer conjugate pH responsive nanoparticle stability; Drug delivery system; Gemcitabine; Polymers; Side effects; pH-responsiveness.

Gemcitabine (GEM) is a powerful anticancer drug for various cancers. However, the anticancer efficacy and the side effects should be addressed for effective therapeutics. To this end, we created a GEM-conjugated polymer (P-GEM) based on cyclic acetal linkage as a delivery carrier of GEM. The obtained P-GEM stably conjugated GEM at physiol. pH (i.e., bloodstream), but released GEM in response to acidic environments such as endosome/lysosome. After systemic administration of P-GEM for mice bearing s.c. tumors, it achieved prolonged blood circulation and enhanced tumor accumulation relative to free GEM system. In addition, the polymer-drug conjugate structure of P-GEM realized effective distribution in the tumor tissues toward the induction of apoptosis in most areas of the tumor sites. Of note, the mol. design of P-GEM achieved minimal accumulation in normal tissues, resulting in negligible GEM-derived adverse effects (e.g., gastrointestinal toxicity and hematotoxicity). Ultimately, even four times smaller dose of P-GEM on a GEM basis realized comparable/higher tumor growth suppression effect for two distinct pancreatic tumor models, compared to free GEM system. The obtained results suggest the huge potential of the present design of GEM-conjugated polymer for anticancer therapeutics.

Biomaterials published new progress about Antitumor agents. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, SDS of cas: 22483-09-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Kong, Jiahui published the artcilePreparation of the key dolutegravir intermediate via MgBr2-promoted cyclization, Synthetic Route of 22483-09-6, the main research area is dolutegravir intermediate preparation; MgBr2-promoted cyclization; chemoselectivity; dolutegravir.

A novel approach for synthesizing the key dolutegravir intermediate is described via MgBr2-promoted intramol. cyclization. Condensation of com. available Me oxalyl chloride and Et 3-(N,N-dimethylamino)acrylate afforded the vinylogous amide in an excellent yield. Subsequent substitution by aminoacetaldehyde di-Me acetal and Me bromoacetate gave rise to the expected precursor for cyclization, which was promoted by MgBr2 to highly selectively convert into pyridinone diester. The key dolutegravir intermediate was finally prepared by the selective hydrolysis of the corresponding diester via LiOH.

Molecules published new progress about Heterocyclization. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Synthetic Route of 22483-09-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Ye, Xiang-Yu published the artcileDesign of oxa-spirocyclic PHOX ligands for the asymmetric synthesis of lorcaserin via iridium-catalyzed asymmetric hydrogenation, Synthetic Route of 22483-09-6, the main research area is oxa spirocyclic phosphine oxazoline PHOX ligand iridium cyclooctadiene preparation; asym hydrogenation catalyst oxa spirocyclic phosphine oxazoline cyclooctadieneiridium preparation; lorcaserin preparation; crystal mol structure bromomethyltetrahydrobenzoazepinone.

Phosphine-oxazoline (PHOX) ligands are a very important class of privileged ligands in asym. catalysis. A series of highly rigid oxa-spiro phosphine-oxazoline (O-SIPHOX) ligands based on O-SPINOL was synthesized efficiently, and their iridium complexes were synthesized by coordination of the O-SIPHOX ligands to [Ir(cod)Cl]2 in the presence of sodium tetrakis-3,5-bis(trifluoromethyl)phenylborate (NaBArF). The cationic iridium complexes showed high reactivity and excellent enantioselectivity in the asym. hydrogenation of 1-methylene-tetrahydro-benzo[d]azepin-2-ones (up to 99% yield and up to 99% ee). A key intermediate of the anti-obesity drug lorcaserin could be efficiently synthesized using this protocol.

Chemical Communications (Cambridge, United Kingdom) published new progress about Crystal structure. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Synthetic Route of 22483-09-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Liu, Y. published the artcileSYNTHESIS AND CHARACTERIZATION OF A NEW COMPOUND 4-(2-CHLOROBENZYL)IMIDAZO[1,2-a] QUINAZOLIN-5(4H)-ONE: DFT STUDY, CRYSTAL STRUCTURE, MEP, AND HOMO-LUMO VALUES, Category: alcohols-buliding-blocks, the main research area is chlorobenzyl imidazolequinazolinone preparation crystal structure DFT.

The new 4-(2-chlorobenzyl)imidazole[1,2-a]quinazolin-5(4H)-one compound was designed, synthesized and used 1H and 13C NMR, FTIR spectroscopy and MS to determine its structure. In addition, the structure of the single crystal was confirmed using X-ray diffraction. The optimal structure of the compound was calculated by DFT using the B3LYP functional group (based on 6-311G(2d,p)) and compared with the structure determined by X-ray diffraction. The results show that the crystal structure determined by X-ray diffraction was consistent with the mol. structure optimized using DFT.

Journal of Structural Chemistry published new progress about Crystal structure. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Category: alcohols-buliding-blocks.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Li, Chenfei published the artcileLuminescent Dinuclear Copper(I) Complexes Bearing an Imidazolylpyrimidine Bridging Ligand, Quality Control of 22483-09-6, the main research area is dinuclear copper imidazolylpyrimidine bridging complex preparation crystal mol structure; phosphorescence luminescence photophysics dinuclear copper imidazolylpyrimidine complex.

The synthesis and photophys. study of two dinuclear copper(I) complexes bearing a 2-(1H-imidazol-2-yl)pyrimidine bridging ligand are described. The tetrahedral coordination sphere of each copper center is completed through the use of a bulky bis(phosphine) ligand, either DPEphos or Xantphos. Temperature-dependent photophys. studies demonstrated emission through a combination of phosphorescence and thermally activated delayed fluorescence for both complexes, and an intense emission (ΦPL = 46%) was observed for a crystalline sample of one of the complexes reported. The photophysics of these two complexes is very sensitive to the environment. Two pseudopolymorphs of one of the dinuclear complexes were isolated, with distinct photophysics. The emission color of the crystals can be changed by grinding, and the differences in their photophysics before and after grinding are discussed.

Inorganic Chemistry published new progress about Crystal structure. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Quality Control of 22483-09-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Uliassi, Elisa published the artcileA Focused Library of Psychotropic Analogues with Neuroprotective and Neuroregenerative Potential, Recommanded Product: 2,2-Dimethoxyethanamine, the main research area is phenothiazin synthesis psychotropic neuroprotectant blood brain barrier neurodegenerative disease; Neurodegenerative diseases; neural regeneration; neuroprotection; phenothiazines; phenotypic screening; psychotropic agents.

Overcoming the lack of effective treatments and the continuous clin. trial failures in neurodegenerative drug discovery might require a shift from the prevailing paradigm targeting pathogenesis to the one targeting simultaneously neuroprotection and neuroregeneration. In the studies reported herein, we sought to identify small mols. that might exert neuroprotective and neuroregenerative potential as tools against neurodegenerative diseases. In doing so, we started from the reported neuroprotective/neuroregenerative mechanisms of psychotropic drugs featuring a tricyclic alkylamine scaffold. Thus, we designed a focused-chem. library of 36 entries aimed at exploring the structural requirements for efficient neuroprotective/neuroregenerative cellular activity, without the manifestation of toxicity. To this aim, we developed a synthetic protocol, which overcame the limited applicability of previously reported procedures. Next, we evaluated the synthesized compounds through a phenotypic screening pipeline, based on primary neuronal systems. Phenothiazine 2Bc showed improved neuroregenerative and neuroprotective properties with respect to reference drug desipramine (2Aa). Importantly, we have also shown that 2Bc outperformed currently available drugs in cell models of Alzheimer’s and Parkinson’s diseases and attenuates microglial activation by reducing iNOS expression.

ACS Chemical Neuroscience published new progress about Alzheimer disease. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Recommanded Product: 2,2-Dimethoxyethanamine.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts