Tag: 200-300

On July 1, 2019, Chen, Chen; Nie, Yiming; Xu, Guangsen; Yang, Xinying; Fang, Hao; Hou, Xuben published an article.Computed Properties of 97-09-6 The title of the article was Design, synthesis and preliminary bioactivity studies of indomethacin derivatives as Bcl-2/Mcl-1 dual inhibitors. And the article contained the following:

Bcl-2 family proteins, which divides into pro-apoptosis proteins and anti-apoptosis proteins, are involved in cell apoptosis progression. As numerous studies illustrated, targeting Bcl-2 family proteins is more and more attractive and practicable to cancer treatment. In this work, we designed and synthesized a series of indomethacin derivatives as new inhibitors for Bcl-2 family proteins. Our results of binding assay to Bcl-2 proteins, MTT assay and apoptotic assay indicated that some compounds had potent binding affinity to Bcl-2/Mcl-1 but not Bcl-xL. Furthermore, compound 8j showed improved anti-proliferative activity than known Bcl-2 inhibitor WL-276. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Computed Properties of 97-09-6

The Article related to apoptosis anticancer bcl2 mcl1 dual inhibitor indomethacin derivative, anticancer, apoptosis, bcl-2/mcl-1 dual inhibitor, indomethacin derivatives, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Computed Properties of 97-09-6

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On June 21, 2021, Gruendler, Franziska; Scholz, Henrik; Herbig, Marcus; Schwarzer, Sandra; Wagler, Jorg; Kroke, Edwin published an article.Formula: C13H12N2O The title of the article was Formation of Aromatic O-Silylcarbamates from Aminosilanes and Their Subsequent Thermal Decomposition with Formation of Isocyanates. And the article contained the following:

A novel phosgene-free route to different isocyanates starts from CO2 and aminosilanes (cf. silylamines) to form so-called carbamoyloxysilanes (O-silylcarbamates), i. e., compounds with the general motif R1R2N-CO-O-SiR3R4R5 as potential precursors. The authors focused on the insertion reaction of CO2 into Si-N bonds of substrates with cyclic (mostly aromatic) amine substituents, i. e., PhNHSiMe3, (PhNH)2SiMe2, PhCH2NHSiMe3, p-(MeO)C6H4NHSiMe3, o-C6H4(NHSiMe3)2, 1,2-C6H10(NHSiMe3)2, o-C6H4(NHSiMe3)(CH2NHSiMe3) and 1,8-C10H6(NHSiMe3)2. Compared to previously studied aminosilanes these reactions are hindered due to the reduced nucleophilicity/basicity of the N-atoms. Whereas slightly increased CO2 pressure (8 bar) and prolonged reaction times (24 h) were sufficient to overcome hindrance of the insertion into, e. g., PhNHSiMe3, intermol. effects in some 2-fold NHSiMe3 functionalized substrates led to partial mono-insertion (e. g., into o-C6H4(NHSiMe3)(CH2NHSiMe3)) or intra-mol. condensation of the intermediate insertion product in case of 1,8-C10H6(NHSiMe3)2 to form 1H-perimidin-2(3H)-one and other side products. Thermal treatment of mono-silylated O-silylcarbamates RHN-CO-O-SiR’3 resulted mainly in the formation of substituted ureas (RHN)2CO, whereas desired isocyanates could not be detected in these cases. Therefore, the authors continued the authors’ studies focussing on N,O-bissilylated precursors, which were obtained by an addnl. N-silylation of the O-silylated carbamates. This allowed the successful formation of isocyanates. As a sole byproduct hexamethyldisiloxane is formed. In all cases, known as well as yet unknown substances were characterized by 1H, 13C and 29Si NMR spectroscopy, along with x-ray diffraction anal. for crystallized solids. The experimental process involved the reaction of 1,3-Diphenylurea(cas: 102-07-8).Formula: C13H12N2O

The Article related to aminosilane insertion reaction carbon dioxide, aromatic silylcarbamate preparation crystal structure, mol structure aromatic silylcarbamate, Organometallic and Organometalloidal Compounds: Silicon Compounds and other aspects.Formula: C13H12N2O

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On May 29, 2012, Uttam, Surana; Krishnan, Vaidehi; Ting, Anthony; Lim, Hong Hwa published a patent.HPLC of Formula: 5455-98-1 The title of the patent was Naphthalamide derivatives having antiproliferative activity. And the patent contained the following:

The invention relates to compounds for use in medicine. The compounds are of general formula (I) as disclosed herein and the pharmaceutically acceptable salts, individual isomers and mixtures of isomers thereof, wherein X, X’ and X are independently O or S; Z is N or P; R3 is optional and is selected from the group consisting of optionally substituted C1-8 alkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6 alkynyl, optionally substituted C1-6 alkoxy, optionally substituted C1-6 thioalkyl, optionally substituted C5-10 aryl, optionally substituted C6-11 alkylaryl, optionally substituted C1-6 alkylamino, optionally substituted C1-6 alkylcarbonyl, optionally substituted C1-6 alkylsulfonamino, optionally substituted (C1-C6)alkylsulfinyl, optionally substituted C1-6 alkylcarbonylamino, optionally substituted hetero(C4-C10)aryl, hydroxyl, halogen, cyano, nitro, amino, formyl, and thiol; R1, R2, R4, R5, R6, R7, R8, R9, and R10 are independently selected from the group consisting of hydrogen, optionally substituted C1-8 alkyl, optionally substituted C2-6 alkenyl, optionally substituted C2-6 alkynyl, optionally substituted C1-6 alkoxy, optionally substituted C1-6 thioalkyl, optionally substituted C5-10 aryl, optionally substituted C6-11 alkylaryl, optionally substituted C1-6 alkylamino, optionally substituted C1-6 alkylcarbonyl, optionally substituted C1-6 alkylsulfonamino, optionally substituted (C1-C6)alkylsulfinyl, optionally substituted C1-6 alkylcarbonylamino, optionall. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).HPLC of Formula: 5455-98-1

The Article related to naphthalamide derivative antiproliferative agent, antitumor agent naphthalamide derivative, antifungal agent naphthalamide derivative, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.HPLC of Formula: 5455-98-1

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On September 15, 2018, Liu, Renshuai; Liu, Lulu; Liu, Tingting; Yang, Xinying; Wan, Yichao; Fang, Hao published an article.Name: 3-Nitro-4-chlorobenzenesulfonamide The title of the article was Discovery and development of substituted tyrosine derivatives as Bcl-2/Mcl-1 inhibitors. And the article contained the following:

Anti-apoptotic Bcl-2 family proteins are vital for cancer cells to escape apoptosis, which make them attractive targets for cancer therapy. Recently, a lead compound I was found to modestly inhibit the binding of BH3 peptide to Bcl-2 protein with a Ki value of 5.2 μM. Based on this, a series of substituted tyrosine derivatives were developed and tested for their binding affinities to Bcl-2 protein. Results indicated that these compounds exhibited potent binding affinities to Bcl-2 and Mcl-1 protein but not to Bcl-XL protein. Promisingly, compound II inhibited the binding of BH3 peptide to Bcl-2 and Mcl-1 protein with a Ki value of 450 and 190 nM resp., and showed obvious anti-proliferative activities against tested cancer cells. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Name: 3-Nitro-4-chlorobenzenesulfonamide

The Article related to tyrosine derivative synthesis anticancer bcl2 mcl1, anti-tumor, apoptosis, bcl-2, mcl-1, tyrosine, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Name: 3-Nitro-4-chlorobenzenesulfonamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On April 30, 2021, Dhumad, Adil M.; Jassem, Ahmed M.; Alharis, Raed A.; Almashal, Faeza A. published an article.Reference of N-((4-Aminophenyl)sulfonyl)acetamide The title of the article was Design, cytotoxic effects on breast cancer cell line (MDA-MB 231), and molecular docking of some maleimide-benzenesulfonamide derivatives. And the article contained the following:

A group of novel maleimide-benzenesulfonamide derivatives 3a-d was designed and synthesized for their evaluation as a potential anti-breast cancer agent. The structures of these derivatives were confirmed by their 1H, 13C NMR, Mass, FT-IR spectral data, and m.ps. The cytotoxic activity (in vitro) of the selected mols. against MDA-MB231 cell line was evaluated by MTT method. Among them, compounds 3a and 3d exhibited a significant cytotoxicity with the IC50 value of 1.61 and 1.26μM, resp., whereas compounds 3b and 3c showed a moderate cytotoxicity with IC50 values of 0.45 and 1.12μM, resp. against MDA-MB231 cells. Docking modeling of the synthesized compounds 3a-d into binding sites of human aromatase protein (PDB ID: 4GL7) was performed to investigate if these derivatives possess analogus binding mode to breast cancer proteins. Docking results showed these compounds have efficient interactions such as hydrogen bonding, Van der Waals interactions, and hydrophobic interactions with the active site residues of the aromatase protein (PDB ID: 4GL7). The low binding energies and a number of hydrogen bonding indicated that the maleimide-benzenesulfonamide derivatives might be considered as a promising anti-breast cancer agent with further developments in drug discovery. The experimental process involved the reaction of N-((4-Aminophenyl)sulfonyl)acetamide(cas: 144-80-9).Reference of N-((4-Aminophenyl)sulfonyl)acetamide

The Article related to maleimide benzenesulfonamide derivative mol docking breast cancer cytotoxicity, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Reference of N-((4-Aminophenyl)sulfonyl)acetamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On January 31, 2013, Mustahil, N. A.; Riyanto, S.; Sukari, M. A.; Rahmani, M.; Mohd nor, S. M.; Ali, A. M. published an article.Related Products of 456-12-2 The title of the article was Antileukemic activity of extracts and constituents of Aegle marmelos. And the article contained the following:

Phytochems. study of various parts of Aegle marmelos (leaves, stem bark and roots) have afforded eleven compounds; hopane and lupane triterpenes including zeorin (1), dustanin (2) also epilupeol (3) and lupenone (4); alkaloids aegeline (5) and skimmianine (6); coumarin derivatives; auraptene (7), epoxyauraptene (8) and marmin (9) together with β-sitosterol and stigmasterol. All crude extracts and isolated compounds were examined for their antileukemic activity against CEM-SS Qmman T-lymphoblastic leukemia cancer cells using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. Roots extracts exhibited significant cytotoxicity while leaves and stem bark extracts were inactive. Hopane triterpenes; zeorin (1) and dustanin (2) as well as alkaloid aegeline (5) isolated from leaves exhibited moderate to strong cytotoxicity with dustanin (2) as the most active constituent (IC50 : 5.3 ± 0.24 μg/mL). Lupane triterpenes; epilupeol (3) and lupenone (4), in addition of coumarin derivative; marmin (9) isolated from stem bark also demonstrated moderate to strong cytotoxicity with epilupeol (3) showed significant activity (IC50 : 6.1 ± 0.20 μg/mL). The chem. constituents isolated from roots were inactive except for epilupeol (3) and marmin (9) which have also been isolated from stem bark. The experimental process involved the reaction of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide(cas: 456-12-2).Related Products of 456-12-2

The Article related to zeorin lupane leaf stem bark root aegle antileukemic, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Related Products of 456-12-2

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Narender, T.; Rajendar, K.; Sarkar, S.; Singh, V. K.; Chaturvedi, Upma; Khanna, A. K.; Bhatia, G. published an article in 2011, the title of the article was Synthesis of novel N-(2-hydroxy-2-p-tolylethyl)-amide and N-(2-oxo-2-p-tolylethyl)-amide derivatives and their antidyslipidemic and antioxidant activity.SDS of cas: 456-12-2 And the article contains the following content:

In continuation of a program on metabolic diseases, the alkaloidal amide aegeline (I) from Aegle marmelos leaves was identified as a dual acting agent (antihyperlipidemic and antihyperglycemic). Therefore, a series of alkaloidal amides [N-(2-hydroxy-2-p-tolylethyl)-amides and N-(2-oxo-2-p-tolylethyl)-amide derivatives] related to aegeline was synthesized and screened in vivo in rats for antihyperlipidemic activity in Triton induced hyperlipidemia model. The synthetic compounds II, (E)-Me-4-C6H4CH(OH)CH2NHCOCH:CHC6H3-4-OH-3-OMe and Me-4-C6H4CH(OH)CH2NHCOCH2R (R = 3-pyridinyl) showed equipotent activity to the natural product, i.e., aegeline. These compounds also showed strong antioxidant activity, which support their antihyperlipidemic activity. Me-4-C6H4COCH2NHCO(CH2)2R (R = 3-pyridinyl) showed better antihyperlipidemic and antioxidant profile than the natural product I. The experimental process involved the reaction of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide(cas: 456-12-2).SDS of cas: 456-12-2

The Article related to aegeline alkaloid amide derivative synthesis antihyperglycemic antidyslipidemic antioxidant activity, Alkaloids: Alkaloids Containing One Nitrogen Atom Not In A Ring and other aspects.SDS of cas: 456-12-2

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On July 31, 2011, Nugroho, Agung Endro; Riyanto, Sugeng; Sukari, Mohamad Aspollah; Maeyama, Kazutaka published an article.Application In Synthesis of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide The title of the article was Effects of aegeline, a main alkaloid of Aegle marmelos correa leaves, on the histamine release from mast cells. And the article contained the following:

Aegeline or N-[2-hydroxy-2(4-methoxyphenyl) ethyl]-3-phenyl-2-propenamide is a main alkaloid isolated from Aegle marmelos Correa collected in Yogyakarta Indonesia. In our study, we investigated the effects of aegeline on the histamine release from mast cell. The study was performed by using (1) rat basophilic leukemia (RBL-2H3) cell line, and (2) rat peritoneal mast cells (RPMCs). DNP24-BSA, thapsigargin, ionomycin, compound 48/80 and PMA were used as inducers for histamine release from mast cell. In our study, aegeline inhibited the histamine release from RBL-2H3 cells induced by DNP24-BSA. Indeed, aegeline showed strong inhibition when RBL-2H3 cells induced by Ca2+ stimulants such as thapsigargin and ionomycin. Aegeline is suggested to influence the intracellular Ca2+ pool only since could not inhibit the 45Ca2+ influx into RBL-2H3 cells. Aegeline showed weak inhibitory effects on the histamine release from RPMCs, even though still succeed to inhibit when the histamine release induced by thapsigargin. These findings indicate that aegeline altered the signaling pathway related to the intracellular Ca2+ pool in which thapsigargin acts. Based on the results, the inhibitory effects of aegeline on the histamine release from mast cells depended on the type of mast cell and also involved some mechanisms related to intracellular Ca2+ signaling events via the same target of the action of thapsigargin or downstream process of intracellular Ca2+ signaling in mast cells. The experimental process involved the reaction of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide(cas: 456-12-2).Application In Synthesis of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide

The Article related to antihistamine aegeline alkaloid aegle leaf histamine release mast cell, Pharmacology: Effects Of Gastrointestinal and Respiratory Drugs and other aspects.Application In Synthesis of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On August 1, 2022, Dabrowska, Aleksandra M.; Mech-Warda, Paulina; Wera, Michal; Domzalska, Marta; Makowski, Mariusz; Chylewska, Agnieszka published an article.Quality Control of N-((4-Aminophenyl)sulfonyl)acetamide The title of the article was Prototropic tautomerism of (E)-N-((4-((2-hydroxy-5-methoxybenzylidene) amino)phenyl)sulfonyl)acetamide and its coordination abilities towards Ru, Rh, and Ir trivalent metal ions. And the article contained the following:

The Schiff base (E)-N-((4-((2-hydroxy-5-methoxybenzylidene)amino)phenyl)sulfonyl) acetamide (ScB-SAM) has been synthesized bytheir condensation at room temperature in ethanol. X-ray crystallog. anal. revealed that the keto-enol tautomerism of its solid state exists as a complex equilibrium system that is stabilized intramol. hydrogen bond. The enol, keto and mixed enol-zwitterionic forms were observed in the crystal structure. The crystallog. results were supported by ATR, and UV-Vis. Phys. properties were determined in different polar and nonpolar solvents and solid state. All above exptl. results were then compared with DFT calculations Addnl., the stabilities of the trivalent: iridium, rhodium and ruthenium ions complexes with ScB-SAM have also been investigated by spectrophotometric titration methods in water. The data showed that the examined coordination compounds were stable in solution based on the values of their stability constants found. The experimental process involved the reaction of N-((4-Aminophenyl)sulfonyl)acetamide(cas: 144-80-9).Quality Control of N-((4-Aminophenyl)sulfonyl)acetamide

The Article related to salicylideneaniline schiff base preparation electronic structure metal coordination stability, Physical Organic Chemistry: Other Reactions, Processes, and Spectra and other aspects.Quality Control of N-((4-Aminophenyl)sulfonyl)acetamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On July 25, 2007, Yu, Xuhui; Ge, Hongyan; Zhang, Lei; Song, Han; Yu, Ying; Wang, Yuhong published an article.Synthetic Route of 456-12-2 The title of the article was Expressions of IL-12 and IL-18 in patients with acute optic neuritis before and after methylprednisolone pulse therapy. And the article contained the following:

The expressions of interleukin-12 (IL-12) and interleukin-18 (IL-18) and the relationship between IL-12 and IL-18 in acute optic neuritis (AON) before and after methylprednisolone pulse therapy (MPPT) were investigated. ELISA was employed to determine the expressions of IL-12 and IL-18 in serum in 27 patients with AON before and after MPPT. RT-PCR anal. was employed to demonstrate the expressions of IL-12 and IL-18 receptors in peripheral lymphocytes. The serum level of IL-12 was decreased from (45.6±12.2) ng/L to (17.1±4.7) ng/L after MPPT (P < 0.01), and that of IL-18 was decreased from (157.5±39.3) ng/L to (126.2±22.6) ng/L (P < 0.05). The expression of IL12R mRNA was decreased after MPPT too (0.2948 vs. 0.1507, P < 0.05), and so was that of IL18R mRNA (0.5352 vs. 0.2843, P < 0.05). The expressions of IL-12 and IL-18 as well as those of their receptors were pos. correlated. Methylprednisolone could exert its important antiphlogistic action against AON by inhibiting the expressions of the proinflammatory cytokines, IL-2 and IL-18. The experimental process involved the reaction of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide(cas: 456-12-2).Synthetic Route of 456-12-2

The Article related to interleukin il12 il18 optic neuritis methylprednisolone antiinflammatory, Mammalian Hormones: Corticosteroid, Gonadal, and Placental Hormones and other aspects.Synthetic Route of 456-12-2

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics