Tag: 0-100

Synthesis and biological evaluation of celastrol derivatives as potent antitumor agents with STAT3 inhibition was written by Xu, Shaohua;Fan, Ruolan;Wang, Lu;He, Weishen;Ge, Haixia;Chen, Hailan;Xu, Wen;Zhang, Jian;Xu, Wei;Feng, Yaqian;Fan, Zhimin. And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2022.Formula: C3H9NO The following contents are mentioned in the article:

Using STAT3 inhibitors as a potential strategy in cancer therapy have attracted much attention. Recently, celastrol has been reported that it could directly bind to and suppress the activity of STAT3 in the cardiac dysfunction model. To explore more effective STAT3 inhibiting anti-tumor drug candidates, we synthesized a series of celastrol derivatives and biol. evaluated them with several human cancer cell lines. The western blotting anal. showed that compound3-Hydroxy-9b,13a-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid 2-(2-thienyl) ethylamide,the most active derivative, could suppress the STAT3s phosphorylation as well as its downstream genes. SPR anal., mol. docking and dynamics simulations results indicated that the 3-Hydroxy-9b,13a-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid 2-(2-thienyl) ethylamide could bind with STAT3 protein more tightly than celastrol. Then we found that the 3-Hydroxy-9b,13a-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid 2-(2-thienyl) ethylamide could block cell-cycle and induce apoptosis on HCT-116 cells. Furthermore, the anti-tumor effect of 3-Hydroxy-9b,13a-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid 2-(2-thienyl) ethylamide was verified on colorectal cancer organoid. This is the first research that discovered effective STAT3 inhibitors as potent anti-tumor agents from celastrol derivatives This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Formula: C3H9NO).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters typically have a pleasant smell; those of low molecular weight are commonly used as fragrances and are found in essential oils and pheromones. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.Formula: C3H9NO

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Discovery and biological evaluation of phthalazines as novel non-kinase TGFβ pathway inhibitors was written by Kharbanda, Anupreet;Zhang, Lingtian;Saha, Debasmita;Tran, Phuc;Xu, Ke;Li, Ming O.;Leung, Yuet-Kin;Frett, Brendan;Li, Hong-yu. And the article was included in European Journal of Medicinal Chemistry in 2021.COA of Formula: C3H9NO The following contents are mentioned in the article:

TGFβ is crucial for the homeostasis of epithelial and neural tissues, wound repair, and regulating immune responses. Its dysregulation is associated with a vast number of diseases, of which modifying the tumor microenvironment is one of vital clin. interest. Despite various attempts, there is still no FDA-approved therapy to inhibit the TGFβ pathway. Major mainstream approaches involve impairment of the TGFβ pathway via inhibition of the TGFβRI kinase. With the purpose to identify non-receptor kinase-based inhibitors to impair TGFβ signaling, an inhouse chem. library was enriched, through a computational study, to eliminate TGFβRI kinase activity. Selected compounds were screened against a cell line engineered with a firefly luciferase gene under TGFβ-Smad-dependent transcriptional control. Results indicated moderate potency for a mol. with phthalazine core against TGFβ-Smad signaling. A series of phthalazine compounds were synthesized and evaluated for potency. The most promising compound I exhibited an IC₅₀ of 0.11 ± 0.02μM and was confirmed to be non-cytotoxic up to 12μM, with a selectivity index of approx. 112-fold. Simultaneously, I was confirmed to reduce the Smad phosphorylation using Western blot without exhibiting inhibition on the TGFβRI enzyme. This study identified a novel small-mol. scaffold that targets the TGFβ pathway via a non-receptor-kinase mechanism. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3COA of Formula: C3H9NO).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters typically have a pleasant smell; those of low molecular weight are commonly used as fragrances and are found in essential oils and pheromones. Because of their lack of hydrogen-bond-donating ability, esters do not self-associate. Consequently, esters are more volatile than carboxylic acids of similar molecular weight.COA of Formula: C3H9NO

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Study the lipidoid nanoparticle mediated genome editing protein delivery using 3D intestinal tissue model was written by Yang, Tao;Han, Haobo;Chen, Ying;Yang, Liu;Parker, Rachael;Li, Yamin;Kaplan, David L.;Xu, Qiaobing. And the article was included in Bioactive Materials in 2021.Safety of 2-Methoxyethylamine The following contents are mentioned in the article:

Lipid nanoparticles are promising carriers for oral drug delivery. For bioactive cargos with intracellular targets, e.g. gene-editing proteins, it is essential for the cargo and carrier to remain complexed after crossing the epithelial layer of intestine in order for the delivery system to transport the cargos inside targeted cells. However, limited studies have been conducted to verify the integrity of cargo/carrier nanocomplexes and their capability in facilitating cargo delivery intracellularly after the nanocomplex crossing the epithelial barrier. Herein, we used a traditional 2D transwell system and a recently developed 3D tissue engineered intestine model and demonstrated the synthetic lipid nanoparticle (carrier) and protein (cargo) nanocomplexes are able to cross the epithelial layer and deliver the protein cargo inside the underneath cells. We found that the EC16-63 LNP efficiently encapsulated the GFP-Cre recombinase, penetrated the intestinal monolayer cells in both the 2D cell culture and 3D tissue models through temporarily interrupting the tight junctions between epithelial layer. After transporting across the intestinal epithelia, the EC16-63 and GFP-Cre recombinase nanocomplexes can enter the underneath cells to induce gene recombination. These results suggest that the in vitro 3D intestinal tissue model is useful for identifying effective lipid nanoparticles for potential oral drug delivery. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Safety of 2-Methoxyethylamine).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits. Esters contain a carbonyl center, which gives rise to 120° C–C–O and O–C–O angles. Unlike amides, esters are structurally flexible functional groups because rotation about the C–O–C bonds has a low barrier. Their flexibility and low polarity is manifested in their physical properties; they tend to be less rigid (lower melting point) and more volatile (lower boiling point) than the corresponding amides. Safety of 2-Methoxyethylamine

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Bamboo pyroligneous acid as a novel insecticide, its mosquito repellency activity, chemical components and safety towards animals was written by Li, Zhikun;Maliang, Huidong;Liu, Qing;Chen, Anliang;Liu, Hongbo;Lin, Haiping;Ma, Jianyi;Wang, Pinwewi. And the article was included in Fresenius Environmental Bulletin in 2022.COA of Formula: C3H9NO The following contents are mentioned in the article:

Mosquitoes transmit pathogens which cause human and mammalian diseases. We employed several practical and multidisciplinary approaches to discover a new natural mosquito repellent. The active ingredient tests revealed that bamboo vinegar (BV) showed 91% protective efficacy. The forearm skin landing test showed that 9% acetic acid water solution (AAWS) and BV had strong protective efficacy against Aedes albopictus. The limb skin landing test also showed that BV and AAWS had protective efficacy. The sugar-feeding behavioral bioassay showed that mosquitoes were repelled by the smell of AAWS. There was no significant difference between the number of mosquitoes that landed on the two Petri dishes treated with BV (6.6% acetic acid (AA)), 4.5% AAWS, 9% AAWS, and 4.5% DEBT, but a significant difference was found among BV (6.6% AA), 4.5% AAWS, 9.0% AAWS, DEBT, and distilled water. The arm-in-cage tests showed that there was a descending order for the duration of complete protection was DEBT (75-90 min) = BV (75-90 min) > formic acid (60-75 min) > AA (45-60 min) > propanoic acid (30-45 min) > butanoic acid (15-30 min) > water (0 min). The safety tests showed that the acute oral toxicity (LD50) of BV (6.6% AA) was > 5000 mg/kg for mice and produced no red spots or edema symptoms. Furthermore, the dermal sensitization rate was zero for rabbits, and the marrow micronucleus rates for mice were neg. In summary, BV can be safely used for volatilization and skin applications. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3COA of Formula: C3H9NO).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Volatile esters with characteristic odours are used in synthetic flavours, perfumes, and cosmetics. Certain volatile esters are used as solvents for lacquers, paints, and varnishes. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.COA of Formula: C3H9NO

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Discovery of quinoline-based proteasome inhibitors for human African trypanosomiasis (HAT) was written by Koester, Dennis C.;Marx, Vanessa M.;Williams, Sarah;Jiricek, Jan;Dauphinais, Maxime;Rene, Olivier;Miller, Sarah L.;Zhang, Lei;Patra, Debjani;Chen, Yen-Liang;Cheung, Harry;Gable, Jonathan;Lakshminarayana, Suresh B.;Osborne, Colin;Galarneau, Jean-Rene;Kulkarni, Upendra;Richmond, Wendy;Bretz, Angela;Xiao, Linda;Supek, Frantisek;Wiesmann, Christian;Honnappa, Srinivas;Be, Celine;Maser, Pascal;Kaiser, Marcel;Ritchie, Ryan;Barrett, Michael P.;Diagana, Thierry T.;Sarko, Christopher;Rao, Srinivasa P. S.. And the article was included in Journal of Medicinal Chemistry in 2022.Category: ethers-buliding-blocks The following contents are mentioned in the article:

Human African Trypanosomiasis (HAT) is a vector-borne disease caused by kinetoplastid parasites of the Trypanosoma genus. The disease proceeds in two stages, with a hemolymphatic blood stage and a meningo-encephalic brain stage. In the latter stage, the parasite causes irreversible damage to the brain leading to sleep cycle disruption and is fatal if untreated. An orally bioavailable treatment is highly desirable. A brain-penetrant, parasite-selective 20S proteasome inhibitor that was rapidly optimized from an HTS singleton hit to drug candidate, I [wherein, X = C, N; R¹ = Me, chloro, bromo; R² = 2-fluoro, 2,3-difluoro, 2,6-difluoro; R³ = cyclopropyl, (2R)-2-fluoro-3-hydroxy-Pr, (2R)-3-hydroxy-2-methoxy-propyl; R⁴ = H; R³R⁴ = C₄H₈], among them I [wherein, X = C, R¹ = chloro, R² = 2,3-difluoro, R³ = (2R)-3-hydroxy-2-methoxy-propyl; R⁴ = H] that showed cure in a stage II mouse efficacy model was reported. Hit expansion and lead optimization campaign guided by cryo-electron microscopy and an in-silico model to predict the brain-to-plasma partition coefficient Kp as an important parameter to prioritize compounds for synthesis was described. The model combined with in-vitro and in-vivo experiments allowed us to advance compounds with favorable unbound brain-to-plasma ratios (Kp,uu) to cure a CNS disease such as HAT. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Category: ethers-buliding-blocks).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Many esters have the potential for conformational isomerism, but they tend to adopt an s-cis (or Z) conformation rather than the s-trans (or E) alternative, due to a combination of hyperconjugation and dipole minimization effects. The preference for the Z conformation is influenced by the nature of the substituents and solvent, if present. Lactones with small rings are restricted to the s-trans (i.e. E) conformation due to their cyclic structure.Category: ethers-buliding-blocks

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Preparation and antimicrobial activities of new piperidine substituted benzothiazole derivatives was written by Shafi, S. Syed;Rajesh, R.;Subaash, R.;Gopinath, S.. And the article was included in Heterocyclic Letters in 2021.Electric Literature of C3H9NO The following contents are mentioned in the article:

Synthesis of piperidine substituted benzothiazole derivatives I [R = 1-piperidyl, (2-methoxyethylamino), (4-bromoanilino), etc.] was reported. The synthesis was done by the reaction of Et 2-aminobenzo[d]thiazole-6-carboxylate with copper (II) bromide followed by the addition of piperidine and get Et 2-(piperidin-1-yl)benzo[d]thiazole-6-caroxylate. The reaction of Et 2-(piperidin-1-yl)benzo[d]thiazole-6-caroxylate with NaOH produced 2-(piperidin-1-yl)benzo[d]thiazole-6-caroxylic acid. The intermediate 2-(piperidin-1-yl)benzo[d]thiazole-6-caroxylic acid was isolated as stable compounds The chem. structures of synthesized compounds were established based on spectral data of ¹H-NMR, ¹³C-NMR, and IR. The mass of the novel compounds was established with the help of the LCMS test. The biol. studies of synthesized compounds I showed that the piperidine, amine, and bromine substituted aniline substituted compounds had good antibacterial activity. The compound amine substituted compound exhibited good antifungal activity. The formation of the crystal was confirmed by powder XRD and the average crystalline size was 54 nm. The photoluminescence data explain the optical property of the compound The biol. studies of synthesized compounds showed that compound I [R = 4-bromoanilino] possesses good antibacterial activity and compound I [R = 2-methoxyethylamino] had good antifungal activity. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Electric Literature of C3H9NO).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits. Acyl chlorides and acid anhydrides alcoholysis is another way to produce esters. Acyl chlorides and acid anhydrides react with alcohols to produce esters. Anydrous conditions are recommended since both acyl chlorides and acid anhydrides react with water.Electric Literature of C3H9NO

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Build-Couple-Transform: A Paradigm for Lead-like Library Synthesis with Scaffold Diversity was written by Uguen, Melanie;Davison, Gemma;Sprenger, Lukas J.;Hunter, James H.;Martin, Mathew P.;Turberville, Shannon;Watt, Jessica E.;Golding, Bernard T.;Noble, Martin E. M.;Stewart, Hannah L.;Waring, Michael J.. And the article was included in Journal of Medicinal Chemistry in 2022.Application In Synthesis of 2-Methoxyethylamine The following contents are mentioned in the article:

High-throughput screening provides one of the most common ways of finding hit compounds Lead-like libraries e.g., I, in particular, provide hits with compatible functional groups and vectors for structural elaboration and phys. properties suitable for optimization. Library synthesis approaches can lead to a lack of chem. diversity because they employ parallel derivatization of common building blocks using single reaction types. This problem through a “build-couple-transform” paradigm for the generation of lead-like libraries e.g., I with scaffold diversity was addressed. Nineteen transformations of 4-oxo-2-butenamides RC(O)CH=CHC(O)N(R¹)R² (R = Ph, 4-methoxyphenyl, tetrahydro-2H-pyran-4-yl, etc.; R¹ = H; R² = 2-methoxyethyl, Bn, 1-methyl-1H-pyrazol-3-yl; R¹R² = -(CH₂)₅-, -(CH₂)₂O(CH₂)₂-) scaffold template were optimized, including 1,4-cyclizations, 3,4-cyclizations, reductions, and 1,4-additions A pool-transformation approach efficiently explored the scope of these transformations for nine different building blocks and synthesized a >170-member library with enhanced chem. space coverage and favorable drug-like properties. Screening revealed hits against CDK2. This work establishes the build-couple-transform concept for the synthesis of lead-like libraries e.g., I and provides a differentiated approach to libraries with significantly enhanced scaffold diversity. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Application In Synthesis of 2-Methoxyethylamine).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits, including apples, durians, pears, bananas, pineapples, and strawberries. Many esters have the potential for conformational isomerism, but they tend to adopt an s-cis (or Z) conformation rather than the s-trans (or E) alternative, due to a combination of hyperconjugation and dipole minimization effects. The preference for the Z conformation is influenced by the nature of the substituents and solvent, if present. Lactones with small rings are restricted to the s-trans (i.e. E) conformation due to their cyclic structure.Application In Synthesis of 2-Methoxyethylamine

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities was written by Zhu, Huajian;Li, Wenlong;Shuai, Wen;Liu, Yang;Yang, Limei;Tan, Yuchen;Zheng, Tiandong;Yao, Hong;Xu, Jinyi;Zhu, Zheying;Yang, Dong-Hua;Chen, Zhe-Sheng;Xu, Shengtao. And the article was included in European Journal of Medicinal Chemistry in 2021.COA of Formula: C3H9NO The following contents are mentioned in the article:

A series of novel N-benzylbenzamide derivatives I (R = dimethylaminyl, piperidin-1-yl, morpholin-4-yl, etc.; R¹ = H, Cl, NO₂, (pyridin-4-ylmethyl)aminyl, etc.; R² = H, NO₂; R³ = (3-hydroxy-4-methoxyphenyl)methyl, (3-fluoro-4-methoxyphenyl)methyl, pyridin-4-ylmethyl, etc.; R⁴ = H, Me), II (X = Y = N, CH) and III were designed and synthesized as tubulin polymerization inhibitors. Among fifty-one target compounds, I, II and III compound I [R = morpholin-4-yl; R¹ = F; R² = H; R³ = (3-hydroxy-4-methoxyphenyl)methyl; R⁴ = H] (IV) exhibited significant antiproliferative activities with IC₅₀ values ranging from 12 to 27 nM against several cancer cell lines, and possessed good plasma stability and satisfactory physicochem. properties. Mechanism studies demonstrated that IV bound to the colchicine binding site and displayed potent anti-vascular activity. Notably, the corresponding disodium phosphate III exhibited an excellent safety profile with the LD₅₀ value of 599.7 mg/kg (i.v. injection), meanwhile, it significantly inhibited tumor growth and decreased microvessel d. in liver cancer cell H22 allograft mouse model without obvious toxicity. Collectively, IV and III are novel promising anti-tubulin agents with more druggable properties and deserve to be further investigated for cancer therapy. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3COA of Formula: C3H9NO).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Esters are more polar than ethers but less polar than alcohols. They participate in hydrogen bonds as hydrogen-bond acceptors, but cannot act as hydrogen-bond donors, unlike their parent alcohols. This ability to participate in hydrogen bonding confers some water-solubility.COA of Formula: C3H9NO

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

A very long-acting parp inhibitor suppresses cancer cell growth in DNA repair-deficient tumor models was written by Fontaine, Shaun D.;Ashley, Gary W.;Houghton, Peter J.;Kurmasheva, Raushan T.;Diolaiti, Morgan;Ashworth, Alan;Peer, Cody J.;Nguyen, Ryan;Figg, William D. Sr.;Beckford-Vera, Denis R.;Santi, Daniel V.. And the article was included in Cancer Research in 2021.Category: ethers-buliding-blocks The following contents are mentioned in the article:

PARP inhibitors are approved for treatment of cancers with BRCA1 or BRCA2 defects. In this study, we prepared and characterized a very long-acting PARP inhibitor. Synthesis of a macromol. prodrug of talazoparib (TLZ) was achieved by covalent conjugation to a PEG_40kDa carrier via a β-eliminative releasable linker. A single injection of the PEG~TLZ conjugate was as effective as ~30 daily oral doses of TLZ in growth suppression of homologous recombination-defective tumors in mouse xenografts. These included the KT-10 Wilms′′ tumor with a PALB2 mutation, the BRCA1-deficient MX-1 triple-neg. breast cancer, and the BRCA2-deficient DLD-1 colon cancer; the prodrug did not inhibit an isogenic DLD-1 tumor with wild-type BRCA2. Although the half-life of PEG~TLZ and released TLZ in the mouse was only ~1 day, the exposure of released TLZ from a single safe, ED of the prodrug exceeded that of oral TLZ given daily over one month. μPET/CT imaging showed high uptake and prolonged retention of an 89Zr-labeled surrogate of PEG~TLZ in the MX-1 BRCA1-deficient tumor. These data suggest that the long-lasting antitumor effect of the prodrug is due to a combination of its long t_1/2, the high exposure of TLZ released from the prodrug, increased tumor sensitivity upon continued exposure, and tumor accumulation. Using pharmacokinetic parameters of TLZ in humans, we designed a long-acting PEG~TLZ for humans that may be superior in efficacy to daily oral TLZ and would be useful for treatment of PARP inhibitor-sensitive cancers in which oral medications are not tolerated. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Category: ethers-buliding-blocks).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Esters contain a carbonyl center, which gives rise to 120° C–C–O and O–C–O angles. Unlike amides, esters are structurally flexible functional groups because rotation about the C–O–C bonds has a low barrier. Their flexibility and low polarity is manifested in their physical properties; they tend to be less rigid (lower melting point) and more volatile (lower boiling point) than the corresponding amides. Category: ethers-buliding-blocks

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Novel Soloxolone Amides as Potent Anti-Glioblastoma Candidates: Design, Synthesis, In Silico Analysis and Biological Activities In Vitro and In Vivo was written by Markov, Andrey V.;Ilyina, Anna A.;Salomatina, Oksana V.;Sen’kova, Aleksandra V.;Okhina, Alina A.;Rogachev, Artem D.;Salakhutdinov, Nariman F.;Zenkova, Marina A.. And the article was included in Pharmaceuticals in 2022.COA of Formula: C3H9NO The following contents are mentioned in the article:

The modification of natural or semisynthetic triterpenoids with amines can be explored as a promising strategy for improving their pharmacol. properties. Here, we report the design and synthesis of 11 novel amide derivatives of soloxolone Me (SM), a cyano enone-bearing derivative of 18βH-glycyrrhetinic acid. Anal. of their bioactivities in vitro and in silico revealed their high toxicity against a panel of tumor cells (average IC50(24h) = 3.7 μM) and showed that the formation of amide moieties at the C-30 position of soloxolone did not enhance the cytotoxicity of derivatives toward tumor cells compared to SM, though it can impart an ability to pass across the blood-brain barrier. Further HPLC-MS/MS and mechanistic studies verified significant brain accumulation of hit compound 12 (soloxolone tryptamide) in a murine model and showed its high anti-glioblastoma potential. It was found that 12 induced ROS-dependent and autophagy-independent death of U87 and U118 glioblastoma cells via mitochondrial apoptosis and effectively blocked their clonogenicity, motility and capacity to form vessel-like structures. Further in vivo study demonstrated that i.p. injection of 12 at a dosage of 20 mg/kg effectively inhibited the growth of U87 glioblastoma in a mouse xenograft model, reducing the proliferative potential of the tumor and leading to a depletion of collagen content and normalization of blood vessels in tumor tissue. The obtained results clearly demonstrate that 12 can be considered as a promising leading compound for drug development in glioblastoma treatment. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3COA of Formula: C3H9NO).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Carboxylic acid esters of low molecular weight are colourless, volatile liquids with pleasant odours, slightly soluble in water. Cyclic esters are called lactones, regardless of whether they are derived from an organic or inorganic acid. One example of an organic lactone is γ-valerolactone.COA of Formula: C3H9NO

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem