Month: November 2022

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

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 January 15, 2017, Ge, Yang; Yang, Haijun; Wang, Changyuan; Meng, Qiang; Li, Lei; Sun, Huijun; Zhen, Yuhong; Liu, Kexin; Li, Yanxia; Ma, Xiaodong published an article.Application of 16230-24-3 The title of the article was Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton’s tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines. And the article contained the following:

A family of phosphoryl-substituted diphenylpyrimidine derivatives (Pho-DPPYs) were synthesized and biol. evaluated as potent BTK inhibitors in this study. Compound 7b was found to markedly inhibit BTK activity at concentrations of 0.82 nmol/L, as well as to suppress the proliferations of B-cell leukemia cell lines (Ramos and Raji) expressing high levels of BTK at concentrations of 3.17 μM and 6.69 μM. Moreover, flow cytometry anal. results further indicated that 7b promoted cell apoptosis to a substantial degree. In a word, compound 7b is a promising BTK inhibitor for the treatment of B-cell lymphoblastic leukemia. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application of 16230-24-3

The Article related to preparation phosphoryl derivative diphenylpyrimidine bruton’s kinase inhibitor leukemia, btk, dppy, inhibitor, leukemia, phosphoryl, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Application of 16230-24-3

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