Category: 97-09-6

Cornwell, E. published an article in 2007, the title of the article was Application of the Vc3 topographic QSPR parameter to benzene sulfonamide derivatives.Application of 97-09-6 And the article contains the following content:

A novel QSPR topog. parameter (Vc3) is used for reduction of the number of independent variables to one variable Vc3, consistent with Euclidian distances relations. This procedure was applied to a model of 19 benzene sulfonamide derivatives, using benzenesulfonamide as a reference The derivatives were characterized by physicochems. properties used as independent variables. The variables are: refraction index, surface tension and an extra dummy variable that indicated the presence or absence chlorine atoms in the mol., while pKa was used like dependent variable. The linear regression proposed is of the form. pKa = m* Vc3 + n, that is more coherent than its counterpart multivariable regression. The use of this variable reduction eliminated problems of orthogonal procedure or the use of Principal Component Anal. (PCA) to obtain consistent models. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Application of 97-09-6

The Article related to qspr benzene sulfonamide derivative, General Organic Chemistry: Other and other aspects.Application of 97-09-6

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

On November 15, 2004, Jaiswal, Mona; Khadikar, Padmakar V.; Supuran, Claudiu T. published an article.COA of Formula: C6H5ClN2O4S The title of the article was Topological modeling of lipophilicity, diuretic activity, and carbonic inhibition activity of benzene sulfonamides: a molecular connectivity approach. And the article contained the following:

A large series of distance-based topol. indexes has been used for modeling lipophilicity, diuretic activity, and carbonic anhydrase inhibition activity of a library of simple substituted benzene sulfonamides. The results have shown that the topol. approach used is quite useful for modeling carbonic anhydrase inhibition and the use of mol. connectivity is the best for this purpose. Excellent results are obtained in multiparametric regressions. The results are critically discussed on the basis of statistical parameters. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).COA of Formula: C6H5ClN2O4S

The Article related to qsar benzene sulfonamide diuretic carbonic anhydrase, Pharmacology: Structure-Activity and other aspects.COA of Formula: C6H5ClN2O4S

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 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

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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 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