Month: November 2022

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 April 30, 2018, Liu, Zhuo; Wang, Luhong; Feng, Min; Yi, Yuanyuan; Zhang, Wenhan; Liu, Wenjuan; Li, Lei; Liu, Zhihao; Li, Yanxia; Ma, Xiaodong published an article.HPLC of Formula: 16230-24-3 The title of the article was New acrylamide-substituted quinazoline derivatives with enhanced potency for the treatment of EGFR T790M-mutant non-small-cell lung cancers. And the article contained the following:

A new class of acrylamide-substituted quinazoline derivatives with enhanced inhibitory activity against mutant EGFR T790M enzyme were synthesized. Among them, compound 10b displayed the strongest inhibitory potency to block the phosphorylation of the EGFR T790M enzyme, with an IC50 value of 4.3 nM. Compared with the lead compound gefitinib, compound 10b significantly strengthened the activity against EGFR T790M (194 times higher). Furthermore, compound 10b only exhibited moderate activity against wild type EGFR, with an IC50 of 105.0 nM, suggesting its improved selectivity over the T790M-mutated EGFR. In addition, compound 10b also showed stronger activity against H1975 cells harboring the EGFR T790M mutation than gefitinib. Moreover, compound 10b has low inhibitory activity toward the normal HBE cells (IC50 > 34.04 μM), indicating its low cell cytotoxicity. Overall, this modification provided a new insight to design covalent binding EGFRT790M inhibitors to prevent 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 acrylamide quinazoline synthesis anticancer egfr lung breast cancer, Pharmacology: Structure-Activity and other aspects.HPLC of Formula: 16230-24-3

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

On March 31, 2018, Beloglazkina, A. A.; Skvortsov, D. A.; Tafeenko, V. A.; Majouga, A. G.; Zyk, N. V.; Beloglazkina, E. K. published an article.Recommanded Product: 27115-50-0 The title of the article was Synthesis and cytotoxicity of novel dispiro derivatives of 5-arylidenoxazolones, potential inhibitors of p53-MDM2 protein-protein interaction. And the article contained the following:

Regioselective synthesis of new dispiro indolinones combining both an indolinone and an oxazolone fragment in their structure comprised the 1,3-dipolar cycloaddition of azomethine ylides, generated in situ from isatin and sarcosine, at 2-aryl-5-arylmethylidene-substituted 1,3-oxazol-5(4H)-ones. When ortho and para halogen atoms were present in the aromatic substituents of the starting oxazolones, complex mixtures containing large amounts of oxazoline ring opening products and their dispiro derivatives were formed. The cytotoxicity of compounds was tested by MTT on LNCaP, PC3, HCT116, MCF7, A549, HEK, and VA13 cell lines. The compound possessing the best cytotoxicity revealed the IC50 = 1.08±0.96 μM towards the p53- expressing LNCaP cells and lower activity (IC50 = 3.21±1.45 μM) towards the non-expressing p53 protein PC3 cells, however, it has proved inactive towards the HCT cells, both expressing (HCT+/+) and non-expressing (HCT-/-) p53. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Recommanded Product: 27115-50-0

The Article related to preparation dispiro derivative arylidenoxazolone p53 mdm2 interaction cancer, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 27115-50-0

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

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

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 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 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 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