Category: 777-44-6

N-Arylsulfonyl Indolines as Retinoic Acid Receptor-Related Orphan Receptor 纬 (ROR纬) Agonists was written by Doebelin, Christelle;Patouret, Remi;Garcia-Ordonez, Ruben D.;Chang, Mi Ra;Dharmarajan, Venkatasubramanian;Kuruvilla, Dana S.;Novick, Scott J.;Lin, Li;Cameron, Michael D.;Griffin, Patrick R.;Kamenecka, Theodore M.. And the article was included in ChemMedChem in 2016.Related Products of 777-44-6 This article mentions the following:

The nuclear retinoic acid receptor-related orphan receptor 纬 (ROR纬; NR1F3) is a key regulator of inflammatory gene programs involved in T helper 17 (T_H17) cell proliferation. As such, synthetic small-mol. repressors (inverse agonists) targeting ROR纬 have been extensively studied for their potential as therapeutic agents for various autoimmune diseases. Alternatively, enhancing T_H17 cell proliferation through activation (agonism) of ROR纬 may boost an immune response, thereby offering a potentially new approach in cancer immunotherapy. Herein the authors describe the development of N-arylsulfonyl indolines as ROR纬 agonists. Structure-activity studies reveal a critical linker region in these mols. as the major determinant for agonism. Hydrogen/deuterium exchange coupled to mass spectrometry (HDX-MS) anal. of ROR纬-ligand complexes help rationalize the observed results. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Related Products of 777-44-6).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Chlorination modifies the physical properties of hydrocarbons in several ways. These compounds are typically denser than water due to the higher atomic weight of chlorine versus hydrogen. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Related Products of 777-44-6

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Activities of 11-Azaartemisinin and N-Sulfonyl Derivatives against Asexual and Transmissible Malaria Parasites was written by Harmse, Rozanne;Coertzen, Dina;Wong, Ho Ning;Smit, Frans J.;van der Watt, Mariette E.;Reader, Janette;Nondaba, Sindiswe H.;Birkholtz, Lyn-Marie;Haynes, Richard K.;N’Da, David D.. And the article was included in ChemMedChem in 2017.HPLC of Formula: 777-44-6 This article mentions the following:

Dihydroartemisinin (DHA), either used in its own right or as the active drug generated in vivo from the other artemisinins in current clin. use-artemether and artesunate-induces quiescence in ring-stage parasites of Plasmodium falciparum (Pf). This induction of quiescence is linked to artemisinin resistance. Thus, we have turned to structurally disparate artemisinins that are incapable of providing DHA on metabolism Accordingly, 11-azaartemisinin 5 and selected N-sulfonyl derivatives were screened against intraerythrocytic asexual stages of drug-sensitive Pf NF54 and drug-resistant K1 and W2 parasites. Most displayed appreciable activities against all three strains, with IC₅₀ values <10.5 nM. The p-trifluoromethylbenzenesulfonyl-11-azaartemisinin derivative 11 [(4′-trifluoromethyl)benzenesulfonylazaartemisinin] was the most active, with IC₅₀ values between 2 and 3 nM. The compounds were screened against Pf NF54 early and transmissible late intraerythrocytic-stage gametocytes using luciferase and parasite lactate dehydrogenase (pLDH) assays. The 2′-thienylsulfonyl derivative 16 (2′-thiophenesulfonylazaartemisinin) was notably active against late-stage (IV-V) gametocytes with an IC₅₀ value of 8.7 nm. All compounds were relatively nontoxic to human fetal lung WI-38 fibroblasts, showing selectivity indexes of >2000 toward asexual parasites. Overall, the readily accessible 11-azaartemisinin 5 and the sulfonyl derivatives 11 and 16 represent potential candidates for further development, in particular for transmission blocking of artemisinin-resistant parasites. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6HPLC of Formula: 777-44-6).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.HPLC of Formula: 777-44-6

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Quinone Reduction by Organo-Osmium Half-Sandwich Transfer Hydrogenation Catalysts was written by Bolitho, Elizabeth M.;Worby, Nathan G.;Coverdale, James P. C.;Wolny, Juliusz A.;Schunemann, Volker;Sadler, Peter J.. And the article was included in Organometallics in 2021.Application of 777-44-6 This article mentions the following:

Organo-osmium(II) 16-electron complexes [Os^II(畏⁶-arene)(R-PhDPEN)] (where 畏⁶-arene = para-cymene or biphenyl) can catalyze the reduction of prochiral ketones to optically pure alcs. in the presence of a hydride source. Such complexes can achieve the conversion of pyruvate to unnatural D-lactate in cancer cells. To improve the catalytic performance of these osmium complexes, we have introduced electron-donor and electron-acceptor substituents (R) into the para (R₁) or meta (R₂) positions of the chiral R-phenyl-sulfonyl-diphenylethylenediamine (R-PhDPEN) ligands and explored the reduction of quinones, potential biol. substrates, which play a major role in cellular electron transfer chains. We show that the series of [Os^II(畏⁶-arene)(R-PhDPEN)] derivatives exhibit high turnover frequencies, enantioselectivities (>92%), and conversions (>93%) for the asym. transfer hydrogenation (ATH) of acetophenone-derived substrates and reduce duroquinone and menadione to their di-alc. derivatives Modeling of the catalysis using d. functional theory (DFT) calculations suggests a mechanism involving formic acid deprotonation assisted by the catalyst amine groups, phenyl-duroquinone stacking, hydride transfer to Os^II, possible CO₂ coordination, and tilting of the 畏⁶-arene ring, followed by hydride transfer to the quinone. These findings not only reveal subtle differences between Ru(II) and Os(II) catalysts, but also introduce potential biol. applications. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Application of 777-44-6).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Chlorination modifies the physical properties of hydrocarbons in several ways. These compounds are typically denser than water due to the higher atomic weight of chlorine versus hydrogen. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Application of 777-44-6

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Manganese-Catalyzed Oxime-Directed ortho-C-H Amidation in Ionic Liquids was written by Kong, Xianqiang;Xu, Bo. And the article was included in Asian Journal of Organic Chemistry in 2019.Application of 777-44-6 This article mentions the following:

An efficient amidation of aromatic oximes RR¹C=NOMe (R = H, Me, Bu; R¹ = Ph, 2-naphthyl, 3-bromophenyl, etc.; RR¹ = tetrahydronaphth-8-yl, 6-methoxytetrahydronaphth-8-yl) via C-H bond activation using readily available sulfonyl azides R²SO₂N₃ (R² = iso-Pr, cyclopropyl, 4-methylphenyl, 2-thiophenyl, 5-dimethylaminonaphth-1-yl, etc.) as amidation reagents has been developed. This reaction is catalyzed by a base metal catalyst system – MnBr(CO)₅/[Hmim]OTf. This method offers excellent chem. yields and regioselectivity with good functional group tolerance. The reusability of MnBr(CO)₅/[Hmim]OTf system makes it relatively practical for large scale C-H amidations. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Application of 777-44-6).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications.While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available. Alkyl chlorides readily undergo attack by nucleophiles.Application of 777-44-6

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Direct C-H Sulfonylimination of Pyridinium Salts was written by Luo, Lihua;Tang, Juan;Sun, Rui;Li, Wenjing;Zheng, Xueli;Yuan, Maoling;Li, Ruixiang;Chen, Hua;Fu, Haiyan. And the article was included in Organic Letters in 2022.Quality Control of 3-(Trifluoromethyl)benzene-1-sulfonyl chloride This article mentions the following:

A direct pyridinium C-H sulfonylimination has been developed for the synthesis of sulfonyl iminopyridine derivatives I (R = H, CN, Ph, thiophen-2-yl, etc.; R¹ = H, OMe, Ph, thiophen-3-yl, etc.; R² = H, cyclopropyl, Ph, 4-bromophenyl, etc.; R¹R² = -CH=CH-CH=CH-; R³ = Me, Et, i-Pr, etc.; R⁴ = Et, Ph, pyridin-3-yl, etc.) with high efficiency. This transformation features the direct and efficient formation of a C=N bond with a high functional group tolerance under metal-free conditions. The spectroscopic properties potentially enable these sulfonyl iminopyridine compounds I to be useful new emitting materials. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Quality Control of 3-(Trifluoromethyl)benzene-1-sulfonyl chloride).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Organic chlorides can cause corrosion in pipelines, valves and condensers, and cause catalyst poisoning. The hydrocarbon processing industry (HPI) and others are affected by damage caused by these substances. Organochlorine compounds are lipophylic, meaning they are more soluble in fat than in water. This gives them a high tenancy to accumulate in the food chain (biomagnification).Quality Control of 3-(Trifluoromethyl)benzene-1-sulfonyl chloride

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Synthesis and antibacterial activity of novel icariin derivatives was written by Wang, A.;Zhang, Aili;Xu, Y.. And the article was included in Pharmazie in 2019.Application In Synthesis of 3-(Trifluoromethyl)benzene-1-sulfonyl chloride This article mentions the following:

A series of aromatic sulfonyls substituted icariin derivatives I (R = 4-FC₆H₄, 4-F₃CC₆H₄, 2-thienyl, etc.) was synthesized and their antibacterial activities against S. aureus (including drug-sensitive bacteria and drug-resistant bacteria) were evaluated. Among them, compound I (R = 4-F₃CC₆H₄) exhibited high potency against methicillin-sensitive (MSSA) and resistant strains of S. aureus (MRSA) with MIC values of 1-2 mmol/L. Reverse virtual screening and mol. docking anal. indicated that compound I (R = 4-F₃CC₆H₄) might bind the allosteric site of PBP2a that may inhibit cell wall synthesis, with the advantage of activity against multidrug resistant S. aureus. Surface plasmon resonance (SPR) experiment further confirmed the binding affinity. Therefore, aromatic sulfonyls at C-3 position substituted icariin derivatives have been considered to be a novel class of anti-MRSA agents worth of further investigation. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Application In Synthesis of 3-(Trifluoromethyl)benzene-1-sulfonyl chloride).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.Application In Synthesis of 3-(Trifluoromethyl)benzene-1-sulfonyl chloride

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

A sulfonamide sialoside analogue for targeting Siglec-8 and -F on immune cells was written by Nycholat, Corwin M.;Duan, Shiteng;Knuplez, Eva;Worth, Charli;Elich, Mila;Yao, Anzhi;O’Sullivan, Jeremy;McBride, Ryan;Wei, Yadong;Fernandes, Steve M.;Zhu, Zhou;Schnaar, Ronald L.;Bochner, Bruce S.;Paulson, James C.. And the article was included in Journal of the American Chemical Society in 2019.Electric Literature of C7H4ClF3O2S This article mentions the following:

The Siglec family of cell surface receptors have emerged as attractive targets for cell-directed therapies due to their restricted expression on immune cells, endocytic properties, and ability to modulate receptor signaling. Human Siglec-8, for instance, has been identified as a therapeutic target for the treatment of eosinophil and mast cell disorders. A promising strategy to target Siglecs involves the use of liposomal nanoparticles with a multivalent display of Siglec ligands. A key challenge for this approach is the identification of a high affinity ligand for the target Siglec. Here, we report the development of a ligand of Siglec-8 and its closest murine functional orthologue Siglec-F that is capable of targeting liposomes to cells expressing Siglec-8 or -F. A glycan microarray library of synthetic 9-N-sulfonyl sialoside analogs was screened to identify potential lead compounds The best ligand, 9-N-(2-naphthyl-sulfonyl)-Neu5Ac伪2-3-[6-O-sulfo]-Gal尾1-4GlcNAc (6′-O-sulfo ^NSANeu5Ac) combined the lead 2-naphthyl sulfonyl C-9 substituent with the preferred sulfated scaffold. The ligand 6′-O-sulfo ^NSANeu5Ac was conjugated to lipids for display on liposomes to evaluate targeted delivery to cells. Targeted liposomes showed strong in vitro binding/uptake and selectivity to cells expressing Siglec-8 or -F and, when administered to mice, exhibit in vivo targeting to Siglec-F⁺ eosinophils. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Electric Literature of C7H4ClF3O2S).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Organic chlorides can be used in production of: PVC, pesticides, chloromethane, teflon, insulators. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.Electric Literature of C7H4ClF3O2S

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Synthesis and identification of novel berberine derivatives as potent inhibitors against TNF-α-induced NF-κB activation was written by Wang, Yan-Xiang;Liu, Lu;Zeng, Qing-Xuan;Fan, Tian-Yun;Jiang, Jian-Dong;Deng, Hong-Bin;Song, Dan-Qing. And the article was included in Molecules in 2017.Related Products of 777-44-6 This article mentions the following:

Twenty-three new berberine (BBR) analogs containing substituents on ring D, I [R¹ = OMe, NH₂, cyclopropanecarbonyloxy, (4-nitrophenyl)sulfonyloxy, etc., R² = OMe, (adamantan-1-yl)acetoxy, (adamantane-10-carbonyloxy)], were synthesized and evaluated for their activity for suppression of tumor necrosis factor (TNF)-α-induced nuclear factor (NF)-κB activation. Structure-activity relationship (SAR) anal. indicated that suitable tertiary/quaternary carbon substitutions at the 9-position or a rigid fragment at position 10 might be beneficial for enhancing their anti-inflammatory potency. Among them, compounds I [R¹ = (1-methylcyclohexane-1-carbonyl)oxy, 2-(bicyclo[2.2.1]heptan-2-yl)acetoxy, (2′-propylpentanoyl)oxy, (p-tert-butylbenzoyl)oxy, R² = OMe] exhibited satisfactory inhibitory potency against NF-κB activation, with an inhibitory rate of around 90% (5 μM), much better than BBR. A preliminary mechanism study revealed that all of them could inhibit TNF-α-induced NF-κB activation via impairing IκB kinase (IKK) phosphorylation as well as cytokines interleukin (IL)-6 and IL-8 induced by TNF-α. Therefore, the results provided powerful information on further structural modifications and development of BBR derivatives into a new class of anti-inflammatory candidates for the treatment of inflammatory diseases. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Related Products of 777-44-6).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Related Products of 777-44-6

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

A whole-animal platform to advance a clinical kinase inhibitor into new disease space was written by Sonoshita, Masahiro;Scopton, Alex P.;Ung, Peter M. U.;Murray, Matthew A.;Silber, Lisa;Maldonado, Andres Y.;Real, Alexander;Schlessinger, Avner;Cagan, Ross L.;Dar, Arvin C.. And the article was included in Nature Chemical Biology in 2018.Synthetic Route of C7H4ClF3O2S This article mentions the following:

Synthetic tailoring of approved drugs for new indications is often difficult, as the most appropriate targets may not be readily apparent, and therefore few roadmaps exist to guide chem. Here, we report a multidisciplinary approach for accessing novel target and chem. space starting from an FDA-approved kinase inhibitor. By combining chem. and genetic modifier screening with computational modeling, we identify distinct kinases that strongly enhance (‘pro-targets’) or limit (‘anti-targets’) whole-animal activity of the clin. kinase inhibitor sorafenib in a Drosophila medullary thyroid carcinoma (MTC) model. We demonstrate that RAF-the original intended sorafenib target-and MKNK kinases function as pharmacol. liabilities because of inhibitor-induced transactivation and neg. feedback, resp. Through progressive synthetic refinement, we report a new class of ‘tumor calibrated inhibitors’ with unique polypharmacol. and strongly improved therapeutic index in fly and human MTC xenograft models. This platform provides a rational approach to creating new high-efficacy and low-toxicity drugs. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Synthetic Route of C7H4ClF3O2S).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Synthetic Route of C7H4ClF3O2S

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Design, synthesis and evaluation of novel (S)-tryptamine derivatives containing an allyl group and an aryl sulfonamide unit as anticancer agents was written by Guo, Zhenbo;Xu, Yiming;Peng, Yujie;Haroon ur Rashid;Quan, Wei;Xie, Peng;Wu, Lichuan;Jiang, Jun;Wang, Lisheng;Liu, Xu. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2019.Synthetic Route of C7H4ClF3O2S This article mentions the following:

A series of (S)-tryptamine derivatives containing an allyl group and an aryl sulfonamide unit, I (R = Ph, 3-Cl-4-FC₆H₃, 4-Br-2-ClC₆H₄, etc.) and II [R = Ph, 2,4,6-(Me₂CH)₃C₆H₂], were designed, synthesized and evaluated for their potential application as anticancer agents. The structures of the synthesized compounds were characterized by ¹H NMR, ¹³C NMR and ESI-MS spectral analyses. The target compounds were evaluated for their in vitro cytotoxicity against HepG2, HeLa, CNE1 and A549 human cancer cell lines. Some of the synthesized compounds showed moderate to good anticancer activities against four selected cancer cell lines, among of which I [R = 2,4,6-(Me₂CH)C₆H₂] (III) was found to be the most active analog possessing IC₅₀ values 16.5-18.7 μM. Further mechanism studies revealed that compound III could significantly induce HepG2 cell cycle arrest at G1 phase, promote cell apoptosis, and inhibit the colony formation as well. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Synthetic Route of C7H4ClF3O2S).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications. The haloform reaction, using chlorine and sodium hydroxide, is also able to generate alkyl halides from methyl ketones, and related compounds. Chloroform was formerly produced thus.Synthetic Route of C7H4ClF3O2S

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics