Category: amides-buliding-blocks

Rawat, Taniya; Uniyal, Sushmita published an article in 2021, the title of the article was A review on phytoconstituents and reported pharmacological activities of rutaceae family plant: Aegle marmelos (L.) correa leaf.Reference of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide And the article contains the following content:

A review. The only plant in the genus Aegle is bael, a slow-growing, resistant subtropical spiky tree. Family: Rutaceae (Citrus family). It’s also known as wood apple, Bengal quince, golden apple, Indian quince, holy fruit, and stone apple in English. In Sanskrit-Bilwa and in Hindi-Bael, bel. The leaf is one of the plant’s most accumulative sections, holding bioactive substances that are generated as secondary metabolites. Traditionally bael is effective in the treatment of dropsy, diarrhoea, dysentery, and intestinal problems. Phenol, flavonoid, tannin, carbohydrate, sterols, Saponin and alkaloid are all found in leaf extract Skimmianine, Aegeline, lupeol, cineol, eugenol, cuminaldehyde, marmesinine, citronella, and essential oils are isolated compounds from bael. The main components were limonene (82.4%) and (Z)-ocimene (5.1%), which together made up 87.5 percent of the leaf oil. Limonene has been shown to be a useful marker for identifying Aegle marmelos oil samples. Reported pharmacol. studies of A.marmelos leaf extract are Learning and memory, Anxiolytic and Antidepressant, Anticonvulsant, Analgesic, Antipyretic, Anti-inflammatory, Immunomodulatory, hepatoprotective, Cardioprotective, Nephrotoxicity, Antiulcer, Antidiarrhoeal, Antimicrobial, Antiobesity, Anti-proliferative, Antidiabetic, Poly cystic ovarian syndrome, Antithroid activity. The experimental process involved the reaction of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide(cas: 456-12-2).Reference of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide

The Article related to review aegle phytoconstituent drug, Plant Biochemistry: Reviews and other aspects.Reference of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide

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

On November 30, 2018, Duan, Gaigai; Fang, Hong; Huang, Chaobo; Jiang, Shaohua; Hou, Haoqing published an article.Synthetic Route of 685-91-6 The title of the article was Microstructures and mechanical properties of aligned electrospun carbon nanofibers from binary composites of polyacrylonitrile and polyamic acid. And the article contained the following:

High mech. performance carbon nanofibers are highly required for the carbon nanofiber-reinforced composites, and it is necessary to develop novel precursors for the preparation of carbon nanofibers. Blends of poly(acrylonitrile-Bu acrylate mono-Bu itaconate) (co-PAN) and polyamic acid (PAA) were electrospun into aligned nanofibers and the nanofibers were converted to carbon nanofibers by thermal imidization, pre-oxidation, and high-temperature carbonization. FT-IR spectroscopy was applied to monitor the chem. structures of the nanofibers before and after pre-oxidation Tensile tests were used to characterize the mech. properties of electrospun carbon nanofibers (ECNFs). The microstructures of ECNFs were investigated by high-resolution TEM and Raman spectroscopy. The ECNFs derived from blend of co-PAN/PAA with molar ratio of 6/4 and with carbonization temperature of 1400° possessed the highest tensile strength of 1212 MPa, which could be attributed to the ordered graphitic structures in ECNFs. The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).Synthetic Route of 685-91-6

The Article related to microstructure mech property carbon nanofiber polyacrylonitrile polamate, Ceramics: Carbon Products and other aspects.Synthetic Route of 685-91-6

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

On June 30, 2021, Ma, Xinyan; Zhang, Ying; Guan, Mingyang; Zhang, Weidong; Tian, Huifang; Jiang, Caixiao; Tan, Xiaoxin; Kang, Weijun published an article.Electric Literature of 79-07-2 The title of the article was Genotoxicity of chloroacetamide herbicides and their metabolites in vitro and in vivo. And the article contained the following:

The toxicity of chloroacetamide herbicide in embryo development remains unclear. Acetochlor (AC) is a chloroacetamide that metabolizes into 2-ethyl-6-methyl-2-chloroacetanilide (CMEPA) and 6-ethyl-o-toluidine (MEA). The present study determined the potential effect of AC and its metabolites on embryo development. Both HepG2 cells and zebrafish embryos were exposed to AC, CMEPA and MEA in the presence or absence of co treatment with anti reactive oxygen species (ROS) reagent N acetylcysteine. The generation of ROS, levels of superoxide dismutase (SOD) and glutathione (GSH) in HepG2 cells and lactate dehydrogenase (LDH) leakage from HepG2 cells were investigated. The effects of AC, CMEPA and MEA on DNA breakage, MAPK/ERK pathway activity, viability and apoptosis of HepG2 cells were examined by comet assay, western blotting, MTT assay and flow cytometry, resp. Levels of LDH, SOD and GSH in zebrafish embryos exposed to AC, CMEPA and MEA were measured. The hatching and survival rates of zebrafish embryos exposed to AC, CMEPA and MEA, were determined, and apoptosis of hatched fish was investigated using acridine orange staining. The present data showed AC, CMEPA and MEA induced generation of ROS and decreased levels of SOD and GSH in HepG2 cells, which in turn promoted DNA breakage and LDH leakage from cells, ultimately inhibiting cell viability and inducing apoptosis, as well as phosphorylation of JNK and P38. However, co treatment with N-acetylcysteine alleviated the pro apoptosis effect of AC and its metabolites. Moreover, exposure to AC, CMEPA and MEA lead to toxicity of zebrafish embryos with decreased SOD and GSH and increased LDH levels and cell apoptosis, ultimately decreasing the hatching and survival rates of zebrafish, all of which was attenuated by treatment with N-acetylcysteine. Therefore, AC and its metabolites (CMEPA and MEA) showed cytotoxicity and embryo development toxicity. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Electric Literature of 79-07-2

The Article related to danio embryos liver cancer chloroacetamide herbicides genotoxicity, acetochlor, apoptosis, chloroacetamide herbicide, embryo toxicity, reactive oxygen species, zebrafish, Toxicology: Agrochemical and other aspects.Electric Literature of 79-07-2

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

On October 15, 2017, Xu, Guangsen; Liu, Tingting; Zhou, Yi; Yang, Xinying; Fang, Hao published an article.Product Details of 97-09-6 The title of the article was 1-Phenyl-1H-indole derivatives as a new class of Bcl-2/Mcl-1 dual inhibitors: Design, synthesis, and preliminary biological evaluation. And the article contained the following:

Bcl-2 proteins, such as B-cell lymphoma (Bcl-2) protein, myeloid cell leukemia sequence 1 (Mcl-1) protein, has been implicated in the progression and survival of multiple tumor types and become a validated and attractive target for cancer therapy. In this work, a series of 1-phenyl-1H-indole derivatives has been designed and synthesized. The preliminary biol. studies (binding assay for Bcl-2 proteins and MTT assay) suggested that some active compounds showed potent inhibitory activities on Bcl-2/Mcl-1 without binding on Bcl-XL. Furthermore, Compound I and II showed better anti-proliferative activity than WL-276. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Product Details of 97-09-6

The Article related to phenylindole synthesis antitumor bcl2 mcl1, 1-phenyl-1h-indole derivatives, anti-tumor, apoptosis, bcl-2/mcl-1 dual inhibition, Pharmacology: Structure-Activity and other aspects.Product Details of 97-09-6

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

On January 1, 2017, Wan, Yichao; Liu, Tingting; Li, Xiaoxian; Chen, Chen; Fang, Hao published an article.Category: amides-buliding-blocks The title of the article was Improved binding affinities of pyrrolidine derivatives as Mcl-1 inhibitors by modifying amino acid side chains. And the article contained the following:

As an important member of anti-apoptotic Bcl-2 protein, myeloid cell leukemia sequence 1 (Mcl-1) protein is an attractive target for cancer therapy. In this study, a new series of pyrrolidine derivatives as Mcl-1 inhibitors were developed by mainly modifying the amino acid side chain of compound 1. Among them, compound 18 (Ki = 0.077 μM) exhibited better potent inhibitory activities towards Mcl-1 protein compared to pos. control Gossypol (Ki = 0.18 μM). In addition, compound 40 possessed good antiproliferative activities against PC-3 cells (Ki = 8.45 μM), which was the same as pos. control Gossypol (Ki = 7.54 μM). The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Category: amides-buliding-blocks

The Article related to pyrrolidine derivative preparation sar mcl1 inhibitor bcl2 apoptosis cancer, bcl-2, cancer, mcl-1, pyrrolidine, target, Pharmacology: Structure-Activity and other aspects.Category: amides-buliding-blocks

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

On July 31, 2019, Liu, Renshuai; Liu, Lulu; Yang, Xinying; Fang, Hao published an article.Recommanded Product: 97-09-6 The title of the article was Discovery and development of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as Bcl-2/Mcl-1 inhibitors. And the article contained the following:

Bcl-2 family proteins play a vital role for cancer cell in escaping apoptosis, and small-mol. anti-apoptotic Bcl-2 protein inhibitors have been developed as new anticancer therapies. In current study, a series of substituted 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives were developed based on the lead compound 1 (Ki = 5.2 μM against Bcl-2 protein). The fluorescence polarization assays suggested that active compounds possessed potent binding affinities to both Bcl-2 and Mcl-1 protein, but had minor or no binding affinities to Bcl-XL protein. MTT assays showed that these compounds had certain anti-proliferative activities against cancer cells. Furthermore, it was found that active compound 11t(I) could induce cell apoptosis and caspase-3 activation in a dose-dependent manner in Jurkat cells. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Recommanded Product: 97-09-6

The Article related to neoplasm antitumor bcl2 mcl1, 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, anti-tumor, apoptosis, bcl-2, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 97-09-6

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

On December 15, 2015, Wan, Yichao; Wang, Junhua; Sun, Feng-e; Chen, Minglu; Hou, Xuben; Fang, Hao published an article.Formula: C6H5ClN2O4S The title of the article was Design, synthesis and preliminary biological studies of pyrrolidine derivatives as Mcl-1 inhibitors. And the article contained the following:

Antiapoptotic proteins, such as B-cell lymphoma (Bcl-2) protein, myeloid cell leukemia sequence 1 (Mcl-1) protein, are potential targets for cancer treatment. In the studies, a series of pyrrolidine derivatives were developed as potent Mcl-1 inhibitors. The preliminary biol. studies suggested that most of target compounds exhibit good abilities for targeting Mcl-1 protein. Among them, compound I (Ki = 0.53 μM) exhibited equal inhibitory activities towards Mcl-1 protein compared to pos. control gossypol (Ki = 0.39 μM). This compound also possessed good antiproliferative activities against MDA-MB-231 and PC-3 cancer cells. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Formula: C6H5ClN2O4S

The Article related to preparation pyrrolidine antitumor neoplasm, anti-tumor, apoptosis, bcl-2, mcl-1, pyrrolidine, Pharmacology: Structure-Activity and other aspects.Formula: C6H5ClN2O4S

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

On February 9, 2006, Wendt, Michael D.; Shen, Wang; Kunzer, Aaron; McClellan, William J.; Bruncko, Milan; Oost, Thorsten K.; Ding, Hong; Joseph, Mary K.; Zhang, Haichao; Nimmer, Paul M.; Ng, Shi-Chung; Shoemaker, Alexander R.; Petros, Andrew M.; Oleksijew, Anatol; Marsh, Kennan; Bauch, Joy; Oltersdorf, Tilman; Belli, Barbara A.; Martineau, Darlene; Fesik, Stephen W.; Rosenberg, Saul H.; Elmore, Steven W. published an article.Reference of 3-Nitro-4-chlorobenzenesulfonamide The title of the article was Discovery and Structure-Activity Relationship of Antagonists of B-Cell Lymphoma 2 Family Proteins with Chemopotentiation Activity in Vitro and in Vivo. And the article contained the following:

Development of a rationally designed potentiator of cancer chemotherapy, via inhibition of Bcl-XL function, is described. Lead compounds generated by NMR screening and directed parallel synthesis displayed sub-μM binding but were strongly deactivated in the presence of serum. The dominant component of serum deactivation was identified as domain III of human serum albumin (HSA); NMR solution structures of inhibitors bound to both Bcl-XL and HSA domain III indicated two potential optimization sites for separation of affinities. Modifications at both sites resulted in compounds with improved Bcl-XL binding and greatly increased activity in the presence of human serum, culminating in 73R, which bound to Bcl-XL with a Ki of 0.8 nM. In a cellular assay 73R reversed the protection afforded by Bcl-XL overexpression against cytokine deprivation in FL5.12 cells with an EC50 of 0.47 μM. 73R showed little effect on the viability of the human non small cell lung cancer cell line A549. However, consistent with the proposed mechanism, 73R potentiated the activity of paclitaxel and UV irradiation in vitro and potentiated the antitumor efficacy of paclitaxel in a mouse xenograft model. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Reference of 3-Nitro-4-chlorobenzenesulfonamide

The Article related to bcl2 family antagonist heterocycle benzenesulfonamide preparation chemopotentiation cancer, Pharmacology: Structure-Activity and other aspects.Reference of 3-Nitro-4-chlorobenzenesulfonamide

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

On January 1, 2018, Ge, Yang; Wang, Changyuan; Song, Shijie; Huang, Jiaxin; Liu, Zhihao; Li, Yongming; Meng, Qiang; Zhang, Jianbin; Yao, Jihong; Liu, Kexin; Ma, Xiaodong; Sun, Xiuli published an article.Application of 16230-24-3 The title of the article was Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. And the article contained the following:

The BTK and JAK3 receptor tyrosine kinases are two validated and therapeutically amenable targets in the treatment of B-cell lymphomas. Here the authors report the identification of several classes of pyrimidine derivatives as potent BTK and JAK3 dual inhibitors. Among these mols., approx. two thirds displayed strong inhibitory capacity at less than 10 nM concentration, and four compounds could significantly inhibit the phosphorylation of BTK and JAK3 enzymes at concentrations lower than 1 nM. Addnl., these pyrimidine derivatives also exhibited enhanced activity to block the proliferation of B-cell lymphoma cells compared with the representative BTK inhibitor ibrutinib. In particular, two structure-specific compounds I and II displayed stronger activity than reference agents in cell-based evaluation, with IC50 values lower than 10 μM. Further biol. studies, including flow cytometric anal., and a xenograft model for in vivo evaluation, also indicated their efficacy and low toxicity in the treatment of B-cell lymphoma. These findings provide a new insight for the development of novel anti-B-cell lymphoma drugs with multitarget actions. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application of 16230-24-3

The Article related to btk jak3 inhibitor antitumor neoplasm, btk, inhibitor, jak3, lymphoma, pyrimidine, Pharmacology: Structure-Activity and other aspects.Application of 16230-24-3

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

On January 26, 2006, Petros, Andrew M.; Dinges, Jurgen; Augeri, David J.; Baumeister, Steven A.; Betebenner, David A.; Bures, Mark G.; Elmore, Steven W.; Hajduk, Philip J.; Joseph, Mary K.; Landis, Shelley K.; Nettesheim, David G.; Rosenberg, Saul H.; Shen, Wang; Thomas, Sheela; Wang, Xilu; Zanze, Irini; Zhang, Haichao; Fesik, Stephen W. published an article.Formula: C6H5ClN2O4S The title of the article was Discovery of a Potent Inhibitor of the Antiapoptotic Protein Bcl-xL from NMR and Parallel Synthesis. And the article contained the following:

The antiapoptotic proteins Bcl-xL and Bcl-2 play key roles in the maintenance of normal cellular homeostasis. However, their overexpression can lead to oncogenic transformation and is responsible for drug resistance in certain types of cancer. This makes Bcl-xL and Bcl-2 attractive targets for the development of potential anticancer agents. Here we describe the structure-based discovery of a potent Bcl-xL inhibitor directed at a hydrophobic groove on the surface of the protein. This groove represents the binding site for BH3 peptides from proapoptotic Bcl-2 family members such as Bak and Bad. Application of NMR-based screening yielded an initial biaryl acid with an affinity (Kd) of ∼300 μM for the protein. Following the classical “SAR by NMR” approach, a second-site ligand was identified that bound proximal to the first-site ligand in the hydrophobic groove. From NMR-based structural studies and parallel synthesis, a potent ligand was obtained, which binds to Bcl-xL with an inhibition constant (Ki) of 36 ± 2 nM. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Formula: C6H5ClN2O4S

The Article related to antiapoptotic protein bclxl inhibitor nmr parallel synthesis structure antitumor, Pharmacology: Structure-Activity and other aspects.Formula: C6H5ClN2O4S

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