Author: Jessica.F

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 July 31, 2018, Zhang, Yinsheng; Gao, Yong; Ren, Jing; Wang, Qinglin; Zhao, Damin; Zhou, Yu; Wu, Zheyang published a patent.Synthetic Route of 16230-24-3 The title of the patent was Preparation of boron-containing compounds as tyrosine kinase inhibitors. And the patent contained the following:

The title compounds I [wherein R1 is H, F, Cl, Br, alkyl, etc.; X is NH or O; R4 and R6 are independently H, alkyl, alkoxy, etc.; R3 and R7 are independently H and alkoxy; R5 is H, alkylamino, alkyl, cycloalkyl, etc.; Cy is (un)substituted Ph] were claimed and prepared The inventive compound has good inhibitory action on tyrosine kinase, and can be applied in treating the proliferative diseases caused by tyrosine kinase. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Synthetic Route of 16230-24-3

The Article related to preparation boron tyrosine kinase inhibitor treatment proliferative disease, Organometallic and Organometalloidal Compounds: Boron Compounds and other aspects.Synthetic Route of 16230-24-3

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 March 12, 2022, Dannatt, Jonathan E.; Yadav, Anshu; Smith, Milton R. III; Maleczka, Robert E. Jr. published an article.Application of 685-91-6 The title of the article was Amide directed iridium C(sp3)-H borylation catalysis with high N-methyl selectivity. And the article contained the following:

A bidentate monoanionic ligand system was developed to enable iridium catalyzed C(sp3)-H activation borylation of N-Me amides. Borylated amides were obtained in moderate to good isolated yields, and exclusive mono-borylation allowed the amide to be the limiting reagent. Selectivity for C(sp3)-H activation was demonstrated in the presence of sterically available C(sp3)-H bonds. Competitive kinetic isotope studies revealed a large primary isotope effect, implicating C-H activation as the rate limiting step. The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).Application of 685-91-6

The Article related to amide directing group iridium catalyst borylation selective bond activation, boronic ester preparation selective, Organometallic and Organometalloidal Compounds: Boron Compounds and other aspects.Application of 685-91-6

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

Yao, Wubing; Yang, Jianguo; Hao, Feiyue published an article in 2020, the title of the article was Ru-Catalyzed Selective C(sp3)-H Monoborylation of Amides and Esters.Reference of N,N-Diethylacetamide And the article contains the following content:

A ruthenium-catalyzed method has been developed for the C(sp3)-H monoborylation of various unactivated alkyl and aryl amides and challenging esters, with a low-cost and bench-stable boron source, providing boronates with exclusive selectivity, high efficiency, and high turnover number (up to 8900). This novel strategy may offer a versatile and environmentally friendly alternative to current methods for selective C(sp3)-H borylation that employ even more expensive metals, such as iridium and rhodium. The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).Reference of N,N-Diethylacetamide

The Article related to green chem ruthenium catalyst selective borylation amide ester, boronic ester preparation green chem, c−h activation, amides, borylation, ester, ruthenium, Organometallic and Organometalloidal Compounds: Boron Compounds and other aspects.Reference of N,N-Diethylacetamide

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

On July 25, 2013, Popovici-Muller, Janeta; Saunders, Jeffrey O.; Salituro, Francesco G.; Cai, Zhenwei; Yan, Shunqi; Zhou, Ding published a patent.HPLC of Formula: 16230-24-3 The title of the patent was Preparation of heterocycles as isocitrate dehydrogenase 1 inhibitors, therapeutically active compositions and their methods of use. And the patent contained the following:

Provided are compounds of formula I as IDH1 inhibitors; their preparation and use of those compounds for treating cancer. Compounds of formula I wherein R1 is (un)substituted C4-6 carbocyclyl; R2 and R3 are independently (un)substituted aryl and (un)substituted heteroaryl; R4 is (un)substituted saturated heterocyclyl, heteroaralkyl, CH2-heterocyclyl, etc.; and pharmaceutically acceptable salts and hydrates thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their IDH1 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of ≤ 0.1 μM. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).HPLC of Formula: 16230-24-3

The Article related to heterocycle preparation idh1 inhibitor treatment cancer, Heterocyclic Compounds (One Hetero Atom): Other 5-Membered Rings and other aspects.HPLC of Formula: 16230-24-3

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

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 August 7, 2018, Wang, Changyuan; Li, Si; Meng, Qiang; Sun, Xiuli; Li, Hua; Shu, Xiaohong; Sun, Huijun; Liu, Kexin; Liu, Zhihao; Ma, Xiaodong published an article.Electric Literature of 16230-24-3 The title of the article was Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines. And the article contained the following:

A new family of diphenylpyrimidine derivatives bearing an amino acid substituent were identified as potent BTK inhibitors. Among them, compound 7b (N-[3-[[5-chloro-2-[4-[2-[2-(methoxycarbonyl)-1-pyrrolidinyl]-2-oxoethoxy]phenylamino]-4-pyrimidinyl]amino]phenyl]-2-acrylamide), which features an L-proline substituent, was identified as the strongest BTK inhibitor, with an IC50 of 8.7 nM. Compound 7b also displayed similar activity against B-cell lymphoma cell lines as ibrutinib. Moreover, 7b exhibited low cytotoxic activity against normal PBMC cells. In addition, the acridine orange/ethidium bromide (AO/EB) staining assay, Western blot anal. and flow cytometry anal. also showed its effectiveness in interfering with B-cell lymphoma cell growth. The mol. simulation performance showed that 7b forms addnl. strong hydrogen bonds with the BTK protein. All these findings provided new clues about the pyrimidine scaffold as an effective BTK inhibitor for the treatment of B-cell lymphoma. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Electric Literature of 16230-24-3

The Article related to diphenylpyrimidine derivative preparation antitumor btk inhibitor b cell lymphoma, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Electric Literature of 16230-24-3

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

On January 31, 2021, Li, Si; Wu, Bin; Zheng, Xu; Wang, Changyuan; Zhao, Jingyuan; Sun, Huijun; Sun, Xiuli; Tang, Zeyao; Yuan, Hong; Chen, Lixue; Ma, Xiaodong published an article.Synthetic Route of 16230-24-3 The title of the article was Synthesis and biological activity of imidazole group-substituted arylaminopyrimidines (IAAPs) as potent BTK inhibitors against B-cell lymphoma and AML. And the article contained the following:

Bruton’s tyrosine kinase (BTK) is a member of the Tec kinase family and plays a key role in the modulation of the B-cell receptor (BCR)-mediated signaling pathway. Inhibition of BTK has been proven to be an effective therapeutic approach for various hematol. malignancies, such as chronic lymphocytic leukemia (CLL), mantle cell leukemia (MCL), diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML). Here, a new series of imidazole group-substituted arylaminopyrimidines (IAAPs) were designed and synthesized as potent inhibitors of the enzymic activity of BTK with a half maximal inhibitory concentration (IC50) ranging from 13.10 to 42.40 nM. In particular, 11a and 11b exhibited stronger antiproliferative activity against AML and B lymphomas cell lines compared with BTK inhibitor ibrutinib and showed low cytotoxicity against normal peripheral blood mononuclear cells (PBMCs). In addition, anal. of the mechanism of action of these compounds revealed that 11a and 11b induced significant apoptosis in AML and B lymphoma cells by arresting the cell cycle at the G1/G0 or G2/M stage and blocked BTK autophosphorylation as well as the ensuing abrogation of pro-survival AKT and ERK signaling. Taken together, these results suggest that 11a and 11b might serve as valuable preclin. candidates for the treatment of AML and B-cell lymphoma. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Synthetic Route of 16230-24-3

The Article related to aml iaap btk inhibitor bcell lymphoma cell cycle akt, aml, b-cell lymphoma, btk inhibitors, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Synthetic Route of 16230-24-3

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