Category: amides-buliding-blocks

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

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 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 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 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 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 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