Tag: 200-300

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 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

On December 31, 2008, Singh, P. P.; Singh, R. B.; Kiran, S.; Tiwari, Anand; Rao, V. Goverdhan published an article.SDS of cas: 97-09-6 The title of the article was QSAR study of sulfonamides as inhibitors of carbonic anhydrase. And the article contained the following:

Quantum chem. reactivity descriptors based QSAR study of 48 sulfonamide derivatives as inhibitors of carbonic anhydrase has been studied in three different sets. The best QSAR model has correlation coefficient above 0.84 in one set the other two sets have the corresponding values above 0.79 and 0.81. The most important descriptor is heat of formation followed by mol. weight and total energy. The combination of descriptors providing the best model are heat of formation, mol. weight, total energy and LUMO energy. The CA enzyme-sulfonamide reaction appears to be favored by energy change. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).SDS of cas: 97-09-6

The Article related to quant structure activity relationship sulfonamide carbonic anhydrase inhibitor, Pharmacology: Structure-Activity and other aspects.SDS of cas: 97-09-6

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

Khadikar, Padmakar V.; Joshi, Ashok; Jaliwala, Yusuf Ali; Joshi, Shoba; Thakral, Gurubhaj Sing published an article in 2007, the title of the article was First study on the use of valence force constant for modeling carbonic anhydrase inhibition robust multiple regression approach.Electric Literature of 97-09-6 And the article contains the following content:

The paper describes the novel use of valence force constant f (S = 0) as a mol. descriptor for modeling carbonic anhydrous (CA) inhibition by benzene sulfonamides using robust multiple regression approach. A variety of statistics are used for this purpose. The paper is the first study which evidence by means of QSAR calculations on isoenzyme-specific features of benzene sulfonamide CA inhibitors. The results have shown that excellent model is obtained in multiparametric regression upon introduction of indicator parameters. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Electric Literature of 97-09-6

The Article related to valence force constant qsar carbonic anhydrase inhibition computational model, Pharmacology: Structure-Activity and other aspects.Electric Literature of 97-09-6

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

Phadni, A.; Sharma, A. S.; Sharma, V.; Khadikar, P. V. published an article in 2012, the title of the article was QSAR study on carbonic anhydrase inhibition activity and related parameters using -SO2NH2 NMR chemical shift and topological indices.Recommanded Product: 3-Nitro-4-chlorobenzenesulfonamide And the article contains the following content:

The QSAR calculations of biol. activities like carbonic anhydrase inhibition, diuretic activity and lgP have been attempted on some sulfonamides using NMR chem. shift of the -SO2NH2 protons and a large set of topol. indexes: the Randic connectivity and the Balaban indexes. Regression anal. shows excellent results in multiparametric modeling. Results indicate that NMR chem. shift can be successfully used for modeling carbonic anhydrase inhibition constant (pki) and diuretic activity (pC), but plays no part in modeling lipophilicity (lg P) of sulfonamides. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Recommanded Product: 3-Nitro-4-chlorobenzenesulfonamide

The Article related to carbonic anhydrase inhibitor qsar sulfonamide lipophilicity diuretic nmr, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 3-Nitro-4-chlorobenzenesulfonamide

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

Chakhtoura, Marita; Fang, Mike; Cubas, Rafael; O’Connor, Margaret H.; Nichols, Carmen N.; Richardson, Brian; Talla, Aarthi; Moir, Susan; Cameron, Mark J.; Tardif, Virginie; Haddad, Elias K. published an article in 2021, the title of the article was Germinal Center T follicular helper (GC-Tfh) cell impairment in chronic HIV infection involves c-Maf signaling.Safety of N-((4-Aminophenyl)sulfonyl)acetamide And the article contains the following content:

We have recently demonstrated that the function of T follicular helper (Tfh) cells from lymph nodes (LN) of HIV-infected individuals is impaired. We found that these cells were unable to provide proper help to germinal center (GC)-B cells, as observed by altered and inefficient anti-HIV antibody response and premature death of memory B cells. The underlying mol. mechanisms of this dysfunction remain poorly defined. Herein, we have used a unique transcriptional approach to identify these mol. defects. We consequently determined the transcriptional profiles of LN GC-Tfh cells following their interactions with LN GC-B cells from HIV-infected and HIV-uninfected individuals, rather than analyzing resting ex-vivo GC-Tfh cells. We observed that proliferating GC-Tfh cells from HIV-infected subjects were transcriptionally different than their HIV-uninfected counterparts, and displayed a significant downregulation of immune- and GC-Tfh-associated pathways and genes. Our results strongly demonstrated that MAF (coding for the transcription factor c-Maf) and its upstream signaling pathway mediators (IL6R and STAT3) were significantly downregulated in HIV-infected subjects, which could contribute to the impaired GC-Tfh and GC-B cell functions reported during infection. We further showed that c-Maf function was associated with the adenosine pathway and that the signaling upstream c-Maf could be partially restored by adenosine deaminase -1 (ADA-1) supplementation. Overall, we identified a novel mechanism that contributes to GC-Tfh cell impairment during HIV infection. Understanding how GC-Tfh cell function is altered in HIV is crucial and could provide critical information about the mechanisms leading to the development and maintenance of effective anti-HIV antibodies. The experimental process involved the reaction of N-((4-Aminophenyl)sulfonyl)acetamide(cas: 144-80-9).Safety of N-((4-Aminophenyl)sulfonyl)acetamide

The Article related to t follicular helper cell chronic hiv infection signalling pathway, Immunochemistry: Immunopathology and other aspects.Safety of N-((4-Aminophenyl)sulfonyl)acetamide

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

On August 19, 2022, York, Edward; McNaughton, Daniel A.; Roseblade, Ariane; Cranfield, Charles G.; Gale, Philip A.; Rawling, Tristan published an article.Application of 102-07-8 The title of the article was Structure-Activity Relationship and Mechanistic Studies of Bisaryl Urea Anticancer Agents Indicate Mitochondrial Uncoupling by a Fatty Acid-Activated Mechanism. And the article contained the following:

Targeting the cancer cell mitochondrion is a promising approach for developing novel anticancer agents. The exptl. anticancer agent N,N’-bis(3,5-dichlorophenyl)urea (SR4) induces apoptotic cell death in several cancer cell lines by uncoupling mitochondrial oxidative phosphorylation (OxPhos) using a protein-free mechanism. However, the precise mechanism by which SR4 depolarizes mitochondria is unclear because SR4 lacks an acidic functional group typically found in protein-independent uncouplers. Recently, it was shown that structurally related thioureas can facilitate proton transport across lipid bilayers by a fatty acid-activated mechanism, in which the fatty acid acts as the site of protonation/deprotonation and the thiourea acts as an anion transporter that shuttles deprotonated fatty acids across the phospholipid bilayer to enable proton leak. In this paper, we show that SR4-mediated proton transport is enhanced by the presence of free fatty acids in the lipid bilayer, indicating that SR4 uncouples mitochondria through the fatty acid-activated mechanism. This mechanistic insight was used to develop a library of substituted bisaryl ureas for structure-activity relationship studies and subsequent cell testing. It was found that lipophilic electron-withdrawing groups on bisaryl ureas enhanced electrogenic proton transport via the fatty acid-activated mechanism and had the capacity to depolarize mitochondria and reduce the viability of MDA-MB-231 breast cancer cells. The most active compound in the series reduced cell viability with greater potency than SR4 and was more effective at inhibiting ATP production The experimental process involved the reaction of 1,3-Diphenylurea(cas: 102-07-8).Application of 102-07-8

The Article related to structure bisaryl urea cancer mitocondrial uncoupling fatty acid, Pharmacology: Structure-Activity and other aspects.Application of 102-07-8

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

On July 23, 2001, Meng, C. Q.; Zheng, X. S.; Holt, L. A.; Hoong, L. K.; Somers, P. K.; Hill, R. R.; Saxena, U. published an article.Quality Control of 3-Nitro-4-chlorobenzenesulfonamide The title of the article was Nitrobenzene Compounds Inhibit Expression of VCAM-1. And the article contained the following:

A series of nitrobenzene compounds has been discovered as potent inhibitors of VCAM-1 expression and, therefore, potential drug candidates for autoimmune and allergic inflammatory diseases. Structure-activity relationship (SAR) studies showed that a nitro group and two other electron-withdrawing groups are essential for these compounds to be potent inhibitors of VCAM-1 expression. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Quality Control of 3-Nitro-4-chlorobenzenesulfonamide

The Article related to nitrobenzene compound structure activity cell adhesion mol vcam1, Pharmacology: Structure-Activity and other aspects.Quality Control of 3-Nitro-4-chlorobenzenesulfonamide

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