Tag: 100-200

Yi, Yuanyuan; Wang, Luhong; Zhao, Dan; Huang, Shanshan; Wang, Changyuan; Liu, Zhihao; Sun, Huijun; Liu, Kexin; Ma, Xiaodong; Li, Yanxia published an article in 2018, the title of the article was Structural optimization of diphenylpyrimidine scaffold as potent and selective epidermal growth factor receptor inhibitors against L858R/T790M resistance mutation in non-small cell lung cancer.HPLC of Formula: 16230-24-3 And the article contains the following content:

A new class of thiodiphenylpyrimidine analogs (Thio-DPPY) were synthesized as potent and selective EGFR T790M inhibitors to overcome gefitinib resistance in non-small cell lung cancer (NSCLC). This structural optimization led to the identification of two potent EGFRT790M/L858R inhibitors, 14a (N-[3-[[5-chloro-2-[4-((1-morpholino)propylthio)phenylamino]-4-pyrimidinyl]amino]phenyl]-2-propenamide) and 14e (N-[3-[[5-chloro-2-[4-((1-morpholino)ethanethioate)phenylamino]-4-pyrimidinyl]oxygen]phenyl]-2-propenamide), which possess IC50 values of 27.5 and 9.1 nM, resp. Moreover, compounds 14a (SI > 36.4) and 14e (SI > 109.9) exhibited high selectivity and low activity against the wild-type EGFR (IC50 > 1000 nM). In particular, compound 14a also displayed strong potency against EGFRT790M-mutated H1975 cells (IC50 = 0.074 μM), but weak activity toward normal cells HBE (IC50 > 40 μM) and LO-2 (IC50 = 9.891 μM). It is important that compound 14a (SI = 52.6) significantly improved the selectivity against mutant H1975 cells over wild-type A431 cells than rociletinib (SI = 6.0), thus revealing its slight cell cytotoxicity. This study provides a promising Thio-DPPY derivative as enhanced EGFR T790M inhibitor, and also revealed valuable clues for further optimization of DPPY scaffold to overcome NSCLC resistance. 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 diphenylpyrimidine preparation egf receptor inhibitor mutation antitumor lung nsclc, egfr t790m, nsclc, inhibitors, pyrimidine, resistance, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.HPLC of Formula: 16230-24-3

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

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 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 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

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 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

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

Nayaka, Swapna r.; Sabari, Anand j. v.; Shareef, Shaik mabu; Usha, N. s. published an article in 2020, the title of the article was Gas chromatography-mass spectroscopy [Gc-Ms] analysis and phytochemical screening for bioactive compounds in Caulerpapeltata(Greenalga).COA of Formula: C6H13NO And the article contains the following content:

Seaweeds (Marine macroalgae) area large group of marine organisms containing important phytochem. constituents with various biol. activities. They are potentially prolific sources of highly bioactivese condary metabolites, which manifest many of the rapeutic effects like anti-cancer, anti-oxidant, anti-inflammatory and anti-diabetic activities. Seaweeds are used by many Asian cultures for traditional medicine preparations The Caulerpapeltata was collected from Rameshwaram coastal area it was shade dried, made in to powder using standardized procedure to get Caulerpa peltata Methanolic Extract (CPME). The phytochems. and Gas Chromatog.-Mass Spectrometry (GC-MS) anal. was done on prepared CPME for identifying the bioactive compounds Phytochem. in vestigation suggests that the Caulerpa peltata exhibited the presence of phytochems. like Alkaloids, Carbohydrates, Phytosterols, Saponins and Diterpenes, which may contribute to its biol. activities. GC-MS anal. showed 28 variety of compounds, among which Dibutylphthalate, n-hexadecanoic acid, and 1,2-Benzenedic arboxylic acid was found in high percentage. The phytochem. studies and the compounds available in GC-MS showed that the Caulerpapeltata contain important bio active compounds, which may have anti-microbial, anti-fungal and anti-canceractivity. Further research is needed for finding its use in development of new pharmaceutical agent and its safe consumption by human for various health benefits. The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).COA of Formula: C6H13NO

The Article related to cauler papeltata bioactive compound phytochem gas chromatog mass spectroscopy, Microbial, Algal, and Fungal Biochemistry: Composition and Products and other aspects.COA of Formula: C6H13NO

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

Nazli, Ibrahim Hanif; Celepci, Duygu Barut; Yakali, Guel; Topkaya, Derya; Ayguen, Muhittin; Alp, Serap published an article in 2018, the title of the article was Spectroscopic, structural and density functional theory (DFT) studies of two oxazol-5-one derivatives.Category: amides-buliding-blocks And the article contains the following content:

In this study, two oxazol-5-one derivatives, C20H20N2O2 (1) and C21H22N2O2 (2), were synthesized by getting condensed p-N,N-diethylaminobenzaldehyde with two presented hippuric acid derivatives and in further studies they were analyzed spectrochem. Mol. and crystal structures of the compounds were determined by single-crystal X-ray diffraction and the results revealed that the mol. packing of the crystal structures were stabilized by weak intraand intermol. interactions also with C-O···π, C-H···π and π···π stacking interactions. Computational studies were also performed using DFT method at B3LYP/6-311G(d,p) level of theory. Vibrational modes and chem. shifts were calculated and compared with the exptl. data. In addition, frontier MOs and mol. electrostatic potential surfaces were simulated. The calculated results show that the optimized geometries can well reproduce the crystal structure. Purpose of this study was to survey the effects of the reactants, which were condensed with each other to produce oxazol-5-one, upon the characteristic properties and crystal forms of the final oxazol-5-one. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Category: amides-buliding-blocks

The Article related to oxazolone condensation reaction hydrogen bond crystal structure, Physical Organic Chemistry: Other Reactions, Processes, and Spectra and other aspects.Category: amides-buliding-blocks

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