Category: 1688-95-5

《A Novel Class of N-Sulfonyl and N-Sulfamoyl Noscapine Derivatives that Promote Mitotic Arrest in Cancer Cells》 was published in ChemMedChem in 2019. These research results belong to Yong, Cassandra; Devine, Shane M.; Gao, Xuexin; Yan, Angelina; Callaghan, Richard; Capuano, Ben; Scammells, Peter J.. Reference of 4-Methyl-1-piperazinesulfonyl Chloride The article mentions the following:

Noscapine displays weak anticancer efficacy and numerous research efforts have attempted to generate more potent noscapine analogs. These modifications included the replacement of the N-Me group in the 6′-position with a range of substituents, where N-ethylcarbamoyl substitution was observed to possess enhanced anticancer activity. Herein, we describe advances in this area, namely the synthesis and pharmacol. evaluation of a series of N-sulfonyl and N-sulfamoyl noscapine derivatives A number of these sulfonyl-containing noscapinoids demonstrated improved activities compared to noscapine. ((R)-5-((S)-4,5-Dimethoxy-1,3-dihydroisobenzofuran-1-yl)-4-methoxy-6-((1-methyl-1H-imidazol-4-yl)sulfonyl)-5,6,7,8-tetrahydro[1,3]dioxolo[4,5-g]isoquinoline) (14 q) displayed sub-micromolar activities of 560, 980, 271 and 443 nM against MCF-7, PANC-1, MDA-MB-435 and SK-MEL-5 cells, resp. This antiproliferative effect was also maintained against drug-resistant NCI/AdrRES cells despite high expression of the multidrug efflux pump, P-glycoprotein. In the experiment, the researchers used many compounds, for example, 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5Reference of 4-Methyl-1-piperazinesulfonyl Chloride)

4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.Reference of 4-Methyl-1-piperazinesulfonyl Chloride

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Computed Properties of C5H11ClN2O2SOn October 12, 2017 ,《Discovery of Novel Macrocyclic Hedgehog Pathway Inhibitors Acting by Suppressing the Gli-Mediated Transcription》 was published in Journal of Medicinal Chemistry. The article was written by Liu, Gang; Huang, Wenjing; Wang, Juan; Liu, Xiaohua; Yang, Jun; Zhang, Yu; Geng, Yong; Tan, Wenfu; Zhang, Ao. The article contains the following contents:

A systemic medicinal chem. campaign was conducted based on a literature hit compound I bearing the 4,5-dihydro-2H-benzo[b][1,5]oxazocin-6(3H)-one core through cyclization of two side substituents of the bicyclic skeleton combined with N-atom walking or ring walking and the central ring expansion or extraction approaches, leading to several series of structurally unique tricyclic compounds Among these, compound II was identified as the most potent against the Hedgehog (Hh) signaling pathway showing an IC50 value of 23 nM. Mechanism studies indicated that compound II inhibited the Hh signaling pathway by suppressing the expression of the transcriptional factors Gli rather than by interrupting the binding of Gli with DNA. We further observed that II was equally potent against both Smo wild type and the two major resistant mutants (Smo D473H and Smo W535L). It potently inhibited the proliferation of medulloblastoma cells and showed significant tumor growth inhibition in the ptch± ;p53-/- medulloblastoma allograft mice model. Though more studies are needed to clarify the precise interaction pattern of II with Gli, its promising in vitro and in vivo properties encourage further profiling as a new-generation Hh signaling inhibitor to treat tumors primarily or secondarily resistant to current Smo inhibitors. In the experimental materials used by the author, we found 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5Computed Properties of C5H11ClN2O2S)

4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.Computed Properties of C5H11ClN2O2S

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Quality Control of 4-Methyl-1-piperazinesulfonyl ChlorideOn November 1, 2019 ,《Photoredox-Catalyzed Generation of Sulfamyl Radicals: Sulfonamidation of Enol Silyl Ether with Chlorosulfonamide》 appeared in Journal of Organic Chemistry. The author of the article were Luo, Qiyu; Mao, Runyu; Zhu, Yan; Wang, Yonghui. The article conveys some information:

A novel and practical photoredox-catalyzed generation of sulfamyl radicals followed by radical sulfonamidation of enol silyl ether has been described. Diverse functionalized β-ketosulfonamides ArCOCH2SO2NRR1 (Ar = 4-MeC6H4, 4-BrC6H4, 2-FC6H4, etc.; R = H, Me, Et, etc.; R1 = H, Me, Et, etc.) were prepared in modest to excellent yields under mild and economic reaction conditions through the present catalytic protocol. Furthermore, the methodol. developed provides an efficient and convenient approach to the synthesis of the antiseizure drug Zonisamide. In the experiment, the researchers used 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5Quality Control of 4-Methyl-1-piperazinesulfonyl Chloride)

4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.Quality Control of 4-Methyl-1-piperazinesulfonyl Chloride

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Muraglia, Ester; Kinzel, Olaf; Gardelli, Cristina; Crescenzi, Benedetta; Donghi, Monica; Ferrara, Marco; Nizi, Emanuela; Orvieto, Federica; Pescatore, Giovanna; Laufer, Ralph; Gonzalez-Paz, Odalys; Di Marco, Annalise; Fiore, Fabrizio; Monteagudo, Edith; Fonsi, Massimiliano; Felock, Peter J.; Rowley, Michael; Summa, Vincenzo published an article on February 28 ,2008. The article was titled 《Design and Synthesis of Bicyclic Pyrimidinones as Potent and Orally Bioavailable HIV-1 Integrase Inhibitors》, and you may find the article in Journal of Medicinal Chemistry.SDS of cas: 1688-95-5 The information in the text is summarized as follows:

HIV integrase is one of the three enzymes encoded by HIV genome and is essential for viral replication, but integrase inhibitors as marketed drugs have just very recently started to emerge. In this study, the evolution from the N-methylpyrimidinone structure to bicyclic pyrimidinones, e.g., I and II, is shown. Introduction of a suitably substituted amino moiety modulated the phys.-chem. properties of the mols. and conferred nanomolar activity in the inhibition of spread of HIV-1 infection in cell culture. An extensive SAR study led to sulfamide I, which inhibited the strand transfer with an IC50 of 7 nM and HIV infection in MT4 cells with a CIC95 of 44 nM, and ketoamide II that inhibited strand transfer with an IC50 of 12 nM and the HIV infection in MT4 cells with a CIC95 of 13 nM and exhibited a good pharmacokinetic profile when dosed orally to preclin. species. The experimental process involved the reaction of 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5SDS of cas: 1688-95-5)

4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.SDS of cas: 1688-95-5

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Liu, Xiaohua; Zhang, Yu; Huang, Wenjing; Tan, Wenfu; Zhang, Ao published an article on January 15 ,2018. The article was titled 《Design, synthesis and pharmacological evaluation of new acyl sulfonamides as potent and selective Bcl-2 inhibitors》, and you may find the article in Bioorganic & Medicinal Chemistry.HPLC of Formula: 1688-95-5 The information in the text is summarized as follows:

The antiapoptotic protein Bcl-2, overexpressed in many tumor cells, is an attractive target for potential small mol. anticancer drug discovery. Herein, we report a different structural modification approach on ABT-263 by merging the piperazinyl-Ph fragment into a bicyclic framework leading to a series of novel analogs, among which tetrahydroisoquinoline 13 was nearly equally potent against Bcl-2 as ABT-263. Further SAR in the P4-interaction pocket afforded the difluoroazetidine substituted analog 55, which retained good Bcl-2 activity with improved Bcl-2/Bcl-xL selectivity. In the experiment, the researchers used many compounds, for example, 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5HPLC of Formula: 1688-95-5)

4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.HPLC of Formula: 1688-95-5

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Synthetic Route of C5H11ClN2O2SOn March 11, 2013, Moukha-chafiq, Omar; Reynolds, Robert C. published an article in ACS Combinatorial Science. The article was 《Parallel Solution-Phase Synthesis of an Adenosine Antibiotic Analog Library》. The article mentions the following:

A library of eighty one adenosine antibiotic analogs was prepared under the Pilot Scale Library Program of the NIH Roadmap initiative from 5′-amino-5′-deoxy-2′,3′-O-isopropylidene-adenosine (I). Diverse aldehyde, sulfonyl chloride and carboxylic acid reactant sets were condensed to I, in solution-phase fashion, leading after acid-mediated hydrolysis to the targeted compounds in good yields and high purity. No marked antituberculosis or anticancer activity was noted on preliminary cellular testing, but these nucleoside analogs should be useful candidates for other types of biol. activity.4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5Synthetic Route of C5H11ClN2O2S) was used in this study.

4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.Synthetic Route of C5H11ClN2O2S

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

《Synthesis and Biological Activity of Sulfonamide Derivatives of Epipodophyllotoxin》 was written by Guianvarc’h, Dominique; Duca, Maria; Boukarim, Chawki; Kraus-Berthier, Laurence; Leonce, Stephane; Pierre, Alain; Pfeiffer, Bruno; Renard, Pierre; Arimondo, Paola B.; Monneret, Claude; Dauzonne, Daniel. Formula: C5H11ClN2O2S And the article was included in Journal of Medicinal Chemistry on April 22 ,2004. The article conveys some information:

A series of novel 4β-substituted sulfonamide derivatives of 4′-O-demethyl-4-desoxypodophyllotoxin, I [R1 = SO2R, R = Me, n-Pr, (CH2)3NH2, 2-thienyl, piperidino, etc.] (II), has been synthesized. II were synthesized by silylating the alc. I (R1 = H), followed by reaction with RSO2Cl, and desilylation. Their effects on human DNA topoisomerase II and, in some cases, on tubulin polymerization were evaluated. Several of the compounds, e.g. II (R = Me), and the synthetic precursor, the 4β-azido compound, are potent topoisomerase II poisons that induce double-stranded breaks in DNA, with either improved or similar activity compared to etoposide. Only the amino precursor, compound I (R1 = H), was slightly active in tubulin polymerization inhibition assays. We observed that the derivatives bearing an aromatic ring on the 4β-sulfonamide substituent were either less cytotoxic or equivalent to the parent drug, while the sulfonamides containing an aliphatic side chain and the amino-sulfonamide derivatives, except II [R = (CH2)15Me, (CH2)3NH2], exhibited increased cytotoxicity compared to etoposide. In vivo, against the P388 leukemia and the A-549 orthotopic model of lung carcinoma, the most promising compounds were the morpholino- and the piperazino-containing sulfonamides derivatives II (R = morpholino, 4-methylpiperazino). In the part of experimental materials, we found many familiar compounds, such as 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5Formula: C5H11ClN2O2S)

4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.Formula: C5H11ClN2O2S

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Zhang, Xin; Lv, Xiao-Qin; Tang, Sheng; Mei, Lin; Li, Ying-Hong; Zhang, Jing-Pu; Jiang, Jian-Dong; Peng, Zong-Gen; Song, Dan-Qing published an article in European Journal of Medicinal Chemistry. The title of the article was 《Discovery and evolution of aloperine derivatives as a new family of HCV inhibitors with novel mechanism》.HPLC of Formula: 1688-95-5 The author mentioned the following in the article:

Aloperine (I), a Chinese natural product with a unique endocyclic scaffold, was first identified to be a potent hepatitis C virus (HCV) inhibitor in our laboratory Thirty-four new aloperine derivatives were designed, synthesized and evaluated for their anti-HCV activities taking I as the lead. Among them, compound II exhibited the potential potency with EC50 values in a micromolar range against both wild-type and direct-acting antiviral agents (DAAs)-resistant variants, and synergistically inhibited HCV replication with approved DAAs. Furthermore, it also owned a good oral pharmacokinetic and safety profile, suggesting a highly druglike nature. The primary mechanism showed that II might target host components, distinctly different from the DAAs currently used in clinic. Therefore, we consider aloperine derivatives to be a novel class of anti-HCV agents, and compound II has been selected as a promising antiviral candidate for further investigation. In the experimental materials used by the author, we found 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5HPLC of Formula: 1688-95-5)

4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.HPLC of Formula: 1688-95-5

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Dow, Robert L.; Paight, Ernest S.; Schneider, Steven R.; Hadcock, John R.; Hargrove, Diane M.; Martin, Kelly A.; Maurer, Tristan S.; Nardone, Nancy A.; Tess, David A.; DaSilva-Jardine, Paul published an article in Bioorganic & Medicinal Chemistry Letters. The title of the article was 《Potent and selective, sulfamide-based human β3-adrenergic receptor agonists》.Name: 4-Methyl-1-piperazinesulfonyl Chloride The author mentioned the following in the article:

A series of sulfamide-based analogs, e.g., I, related to L-796568 were prepared and evaluated for their biol. activity at the human β3-adrenergic receptor (AR). This modification allows for a significant reduction in mol. weight, while maintaining single-digit nanomolar potencies at the β3-AR and high selectivities vs. the β1- or β2-AR.4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5Name: 4-Methyl-1-piperazinesulfonyl Chloride) was used in this study.

4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.Name: 4-Methyl-1-piperazinesulfonyl Chloride

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Prasad, J. V. N. Vara; Markoski, Larry J.; Boyer, Fred E.; Domagala, John M.; Ellsworth, Edmund L.; Gajda, Christopher; Hagen, Susan E.; Tait, Bradley D.; Lunney, Elizabeth A.; Tummino, Peter J.; Ferguson, Donna; Holler, Tod; Hupe, Donald; Nouhan, Carolyn; Gracheck, Stephen J.; VanderRoest, Steven; Saunders, James; Iyer, K.; Sinz, M. published their research in Bioorganic & Medicinal Chemistry Letters on August 2 ,1999. The article was titled 《Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydro-2-pyranones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety》.Product Details of 1688-95-5 The article contains the following contents:

Dihydropyran-2-ones possessing a sulfamate moiety at the 4-position of a phenylthio ring were designed to reach S3′ pocket of the HIV protease. Synthetic routes for the preparation of thiotosylates possessing 3-(2-tert-butyl-5-methyl-4-sulfamate) phenylthio moiety were established. SAR of various sulfamate analogs including HIV protease binding affinities, antiviral activities and therapeutic indexes will be described. An example compound thus prepared and tested was sulfamic acid 4-[[5,6-dihydro-4-hydroxy-6-[2-(4-hydroxyphenyl)ethyl]-6-methyl-2-oxo-2H-pyran-3-yl]thio]-5-(1,1-dimethylethyl)-2-methylphenyl ester. The experimental part of the paper was very detailed, including the reaction process of 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5Product Details of 1688-95-5)

4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.Product Details of 1688-95-5

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics