Category: 22952-32-5

Bourzikat, Otmane; El Abbouchi, Abdelmoula; Ghammaz, Hamza; El Brahmi, Nabil; El Fahime, Elmostfa; Paris, Arnaud; Daniellou, Richard; Suzenet, Franck; Guillaumet, Gerald; El Kazzouli, Said published the artcile< Synthesis, Anticancer Activities and Molecular Docking Studies of a Novel Class of 2-Phenyl-5,6,7,8-tetrahydroimidazo[1,2-b]pyridazine Derivatives Bearing Sulfonamides>, Reference of 22952-32-5, the main research area is arylsulfonyl tetrahydroimidazopyridazine preparation anticancer human mol docking SAR; sulfonyl chloride phenyl tetrahydroimidazopyridazine sulfonylation; 2-phenyl-5,6,7,8-tetrahydroimidazo [1,2-b]pyridazine; anticancer activity; human cancer cell lines; sulfonamides.

New 2-phenyl-5-(arylsulfonyl)-7,8-dihydro-6H-imidazo[1,2-b]pyridazines I [R = 4-MeC6H4, 4-F3CC6H4, 1-naphthyl, etc.] were synthesized via sulfonylation of 2-phenyl-5,6,7,8-tetrahydroimidazo[1,2-b]pyridazine using sulfonyl chlorides. The structures of these derivatives I were elucidated by 1H NMR, 13C NMR, IR and high-resolution mass spectrometry for further characterization and were further evaluated for their anticancer activities. The anticancer activities of compounds I were evaluated against five human cancer cell lines, including A-549, Hs-683, MCF-7, SK-MEL-28 and B16-F10 cell lines with 5-fluorouracil and etoposide as reference drugs. Among the tested compounds, I [R = 5-Cl-2-OMeC6H3, 4-F3CC6H4] exhibited excellent activities in the same range of the pos. controls, 5-fluorouracil and etoposide, against MCF-7 and SK-MEL-28 cancer cell lines, with IC50 values ranging from 1 to 10 μM. The mol. docking studies of compounds, I [R = 5-Cl-2-OMeC6H3, 4-F3CC6H4] showed a strong binding with some kinases, which were linked to MCF-7 and SK-MEL-28 cancer cell lines.

Molecules published new progress about Antitumor agents. 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Reference of 22952-32-5.

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

Ullah, Safi; Saeed, Muhammad; Ullah, Irfan; Halimi, Syed Muhammad Ashhad; Khan, Khalid Mohammed; Jahan, Saqib; Mohani, Syed Nadeem; Khan, Saifullah; Khan, Ajmal published the artcile< Synthesis and characterization of novel piroxicam derivatives and their antiglycation activity>, Product Details of C7H6Cl2O3S, the main research area is piroxicam derivative preparation SAR antiglycation.

A series of sulfonated esters of piroxicam I (R = Me, Et, Ph, etc.) were synthesized by substitution of “”H”” from hydroxyl “”OH”” group of piroxicam with different alkyl/aryl sulfonyl chloride by continuous stirring at room temperature Compounds I were screened for antiglycation activity, in order to analyze the effect of substitution for the management of late diabetic complications. The preliminary results showed that compound I (R = Ph) exhibited potent antiglycation activity far better than the reference (rutin IC50 = 274.5 ± 0.05μM), while compounds I (R = 2,4-(MeO)2C6H3) and I (R = 4-ClC6H4) were similar with IC50 values of 178.9 ± 1.55μM, 237 ± 2.01μM, and 256.5 ± 2.56μM resp. Moreover a neg. effect of electron withdrawing groups was observed over the inhibition potential of different analogs depending upon the number and the positions of the substituents.

Journal of Molecular Structure published new progress about Advanced glycation end product inhibitors. 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Product Details of C7H6Cl2O3S.

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

Xiang, Qiuping; Luo, Guolong; Zhang, Cheng; Hu, Qingqing; Wang, Chao; Wu, Tianbang; Xu, Hongrui; Hu, Jiankang; Zhuang, Xiaoxi; Zhang, Maofeng; Wu, Shuang; Xu, Jinxin; Zhang, Yan; Liu, Jinsong; Xu, Yong published the artcile< Discovery, optimization and evaluation of 1-(indolin-1-yl)ethan-1-ones as novel selective TRIM24/BRPF1 bromodomain inhibitors>, HPLC of Formula: 22952-32-5, the main research area is prostate cancer TRIM24 BRPF1 bromodomain inhibitor structure activity relationship; BRPF1; Bromodomain; Dual targeting inhibitor; Structure-guided design; TRIM24.

TRIM24 (tripartite motif-containing protein 24) and BRPF1 (bromodomain and PHD finger containing protein 1) are epigenetics “”readers”” and potential therapeutic targets for cancer and other diseases. Here we describe the structure-guided design of 1-(indolin-1-yl)ethan-1-ones as novel TRIM24/BRPF1 bromodomain inhibitors. The representative compound 20l (Y08624) is a new TRIM24/BRPF1 dual inhibitor, with IC50 values of 0.98 and 1.16 μM, resp. Cellular activity of 20l was validated by viability assay in prostate cancer (PC) cell lines. In PC xenograft models, 20l suppressed tumor growth (50 mg/kg/day, TGI = 53%) without exhibiting noticeable toxicity. Compound 20l represents a versatile starting point for the development of more potent TRIM24/BRPF1 inhibitors.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, HPLC of Formula: 22952-32-5.

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

Taha, Muhammad; Rahim, Fazal; Khan, Aftab Ahmad; Anouar, El Hassane; Ahmed, Naveed; Shah, Syed Adnan Ali; Ibrahim, Mohamed; Zakari, Zainul Amiruddin published the artcile< Synthesis of diindolylmethane (DIM) bearing thiadiazole derivatives as a potent urease inhibitor>, HPLC of Formula: 22952-32-5, the main research area is indolylmethyl phenylthiadiazolyl arenesulfonamide preparation urease inhibition SAR mol docking.

The synthesis of diindolylmethane (DIM) derivatives based-thiadiazole I [R = Ph, 2,4-dichlorophenyl, 1-naphthyl, etc.] as a new class of urease inhibitors. Diindolylmethane-based-thiadiazole analogs I were synthesized and characterized by various spectroscopic techniques 1HNMR, 13C-NMR, EI-MS and evaluated for urease (jack bean urease) inhibitory potential. All compounds I showed excellent to moderate inhibitory potential having IC50 value within the range of 0.50 ± 0.01 to 33.20 ± 1.20μM compared with the standard thiourea (21.60 ± 0.70μM). Compound I [R = 2,4-dinitrophenyl] (IC50 = 0.50 ± 0.01μM) was the most potent inhibitor amongst all derivatives I. Structure-activity relationships have been established for all compounds I. The key binding interactions of most active compounds with enzyme were confirmed through mol. docking studies.

Scientific Reports published new progress about Arenesulfonyl chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, HPLC of Formula: 22952-32-5.

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

Whalley, David M.; Duong, Hung A.; Greaney, Michael F. published the artcile< A visible light-mediated, decarboxylative, desulfonylative Smiles rearrangement for general arylethylamines syntheses>, Quality Control of 22952-32-5, the main research area is arylethylamine preparation; alanine oxime ester decarboxylative desulfonylative Smiles rearrangement photocatalysis.

A decarboxylative, desulfonylative Smiles rearrangement is presented that employs activated-ester/energy transfer catalysis to decarboxylate β-amino acid derived starting materials at room-temperature under visible light irradiation The radical Smiles rearrangement gives a range of biol. active arylethylamine products highly relevant to the pharmaceutical industry, chem. biol. and materials science. The reaction is then applied to the synthesis of a chiral unnatural amino acid, 2-thienylalanine, used in the treatment of phenylketonuria. It was also shown how the reaction can proceed under metal-free and catalyst-free conditions.

Chemical Communications (Cambridge, United Kingdom) published new progress about Amino acids Role: RCT (Reactant), RACT (Reactant or Reagent). 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Quality Control of 22952-32-5.

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

Canale, Vittorio; Kotanska, Magdalena; Dziubina, Anna; Stefaniak, Matylda; Siwek, Agata; Starowicz, Gabriela; Marciniec, Krzysztof; Kasza, Patryk; Satala, Grzegorz; Duszynska, Beata; Bantreil, Xavier; Lamaty, Frederic; Bednarski, Marek; Sapa, Jacek; Zajdel, Pawel published the artcile< Design, Sustainable Synthesis and Biological Evaluation of a Novel Dual α2A/5-HT7 Receptor Antagonist with Antidepressant-Like Properties>, Synthetic Route of 22952-32-5, the main research area is dihydrobenzofuranoxy ethyl piperidine preparation antidepressant activity green chem SAR; 5-HT7 receptor antagonist; depression; forced swim test; medicinal mechanochemistry; α2 adrenoceptor antagonist.

The complex pathophysiol. of depression, together with the limits of currently available antidepressants, has resulted in the continuous quest for alternative therapeutic strategies. Numerous findings suggest that pharmacol. blockade ofα2-adrenoceptor might be beneficial for the treatment of depressive symptoms by increasing both norepinephrine and serotonin levels in certain brain areas. The antidepressant properties of 5-HT7 receptor antagonists have been widely demonstrated in a large set of animal models. Considering the potential therapeutic advantages in targeting both α2-adrenoceptors and 5-HT7 receptors, a small series of arylsulfonamide derivatives of (dihydrobenzofuranoxy)ethyl piperidines I (Ar = 4-fluorophenyl, naphthalen-1-yl, isoquinolin-4-yl, etc.; m = 0,1) as dually active ligands were designed. Following green chem. principles, the designed compounds were synthesized entirely using a sustainable mechanochem. approach. The identified compound I (Ar = 5-chloro-2-fluorophenyl (II)) behaved as a potent α2A/5-HT7 receptor antagonist and displayed moderate-to-high selectivity over α1-adrenoceptor subtypes and selected serotonin and dopaminergic receptors. Finally, (II) improved performance of mice in the forced swim test, displaying similar potency to the reference drug mirtazapine.

Molecules published new progress about 5-HT antagonists. 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Synthetic Route of 22952-32-5.

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

El Abbouchi, Abdelmoula; El Brahmi, Nabil; Hiebel, Marie-Aude; Bignon, Jerome; Guillaumet, Gerald; Suzenet, Franck; El Kazzouli, Said published the artcile< Synthesis and biological evaluation of ethacrynic acid derivatives bearing sulfonamides as potent anti-cancer agents>, Application In Synthesis of 22952-32-5, the main research area is ethacrynic acid sulfonamide preparation anticancer human safety; Anti-cancer; Anti-proliferative; Cancer cells; Ethacrynic acid; Safety ratios; Sulfonamides.

A series of ethacrynic acid (2-[2,3-dichloro-4-(2-methylidenebutanoyl)phenoxy]acetic acid) (EA, Edecrin) containing sulfonamides linked via three types of linkers namely 1,2-ethylenediamine, piperazine and 4-aminopiperidine was synthesized and subsequently evaluated in vitro against HL60 and HCT116 cancer cell lines. All the EA analogs, excluding two derivs, showed anti-proliferative activity with IC50s in the micromolar range (less than 4 uM). Three derivatives I-III were selected for their interesting dual activity on HL60 cell line in order to be further evaluated against a panel of cancer cell lines (HCT116, A549, MCF7, PC3, U87-MG and SKOV3) as well as on MRC5 as a normal cell line. These compounds displayed IC50 values in nanomolar range against A549, MCF7, PC3 and HCT116 cell lines, deducing the discovery that piperazine or 4-aminopiperidine is the linker’s best choice to develop EA analogs with highly potent anti-proliferative activities own up to 24 nM. Besides, in terms of selectivity, those linkers are more suitable offering safety ratios of up to 63.8.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Application In Synthesis of 22952-32-5.

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

Tian, Maoqun; Abdelrahman, Aliaa; Baqi, Younis; Fuentes, Eduardo; Azazna, Djamil; Spanier, Claudia; Densborn, Sabrina; Hinz, Sonja; Schmid, Ralf; Mueller, Christa E. published the artcile< Discovery and Structure Relationships of Salicylanilide Derivatives as Potent, Non-acidic P2X1 Receptor Antagonists>, Name: 5-Chloro-2-methoxybenzenesulfonyl chloride, the main research area is inflammation P2X1 receptor calcium influx allosteric modulators antagonists.

Antagonists for the ATP-gated ion channel receptor P2X1 have potential as antithrombotics and for treating hyperactive bladder and inflammation. In this study, salicylanilide derivatives were synthesized based on a screening hit. P2X1 antagonistic potency was assessed in 1321N1 astrocytoma cells stably transfected with the human P2X1 receptor by measuring inhibition of the ATP-induced calcium influx. Structure-activity relationships were analyzed, and selectivity vs. other P2X receptor subtypes was assessed. The most potent compounds, N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzamide (1, IC50 0.0192 μM)(I) and N-[3,5-bis(trifluoromethyl)phenyl]-4-chloro-2-hydroxybenzamide (14, IC50 0.0231 μM)(II), displayed >500-fold selectivity vs. P2X2 and P2X3, and 10-fold selectivity vs. P2X4 and P2X7 receptors, and inhibited collagen-induced platelet aggregation. They behaved as neg. allosteric modulators, and mol. modeling studies suggested an extracellular binding site. Besides selective P2X1 antagonists, compounds with ancillary P2X4 and/or P2X7 receptor inhibition were discovered. These compounds represent the first potent, non-acidic, allosteric P2X1 receptor antagonists reported to date.

Journal of Medicinal Chemistry published new progress about Asthma. 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Name: 5-Chloro-2-methoxybenzenesulfonyl chloride.

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

Ajenjo, Javier; Klepetarova, Blanka; Greenhall, Martin; Bim, Daniel; Culka, Martin; Rulisek, Lubomir; Beier, Petr published the artcile< Preparation of (Pentafluorosulfanyl)benzenes by Direct Fluorination of Diaryldisulfides: Synthetic Approach and Mechanistic Aspects>, Recommanded Product: 5-Chloro-2-methoxybenzenesulfonyl chloride, the main research area is pentafluorosulfanyl benzene preparation reaction mechanism radical; fluorine; pentafluorosulfanyl; radical reactions; reaction mechanisms; synthetic methods.

Direct fluorination of ortho-, meta- and para-substituted aromatic thiols and disulfides using elemental fluorine afforded substituted (pentafluorosulfanyl)benzenes ArSF5 [Ar = 4-FC6H4, 2-NCC6H4, 4-HOOCC6H4, etc.]. This work thus represented the first study of the scope and limitation of direct fluorination for the synthesis of new SF5-containing building blocks. Fluorinations in batch and flow modes were compared. A comprehensive computational study was carried out employing d. functional and wave function methods to elucidate the reaction mechanism of the transformation of ArSF3 into ArSF5. Eliminating various nonradical pathways, it was shown that the reaction proceeded by a radical mechanism, initiated by the attack of the F. on the ArSF3 moiety, propagated via an almost barrierless F2+ArSF4.→ArSF5+F. step and terminated by the ArSF4.+F.→ArSF5. Most of the calculated data were in very good agreement with exptl. observations concerning the ortho-substituent effect on the reaction rates and yields.

Chemistry – A European Journal published new progress about Aromatic compounds Role: PRP (Properties), SPN (Synthetic Preparation), PREP (Preparation) ((pentafluorosulfanyl)benzenes). 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Recommanded Product: 5-Chloro-2-methoxybenzenesulfonyl chloride.

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

Rafique, Rafaila; Khan, Khalid Mohammed; Arshia; Chigurupati, Sridevi; Wadood, Abdul; Rehman, Ashfaq Ur; Salar, Uzma; Venugopal, Vijayan; Shamim, Shahbaz; Taha, Muhammad; Perveen, Shahnaz published the artcile< Synthesis, in-vitro α-amylase inhibitory, and radicals (DPPH & ABTS) scavenging potentials of new N-sulfonohydrazide substituted indazoles>, Application In Synthesis of 22952-32-5, the main research area is phenyl tetrahydroindazolone preparation; tetrahydroindazolylidene sulfonohydrazide diastereoselective preparation; amylase inhibition kinetics antioxidant activity SAR docking; ABTS and DPPH; In silico; In vitro; Indazole; Sulfonohydrazide; α-amylase enzyme.

A series of new N-sulfonohydrazide substituted indazoles I and II [R = Me, Ph, 1-naphthyl, etc.] were synthesized by multistep reaction scheme and assessed for in-vitro α-amylase inhibitory and radical (DPPH and ABTS) scavenging properties. All compounds I and II were fully characterized by different spectroscopic techniques including 1H, 13C NMR, EI-MS, HREI-MS, ESI-MS and HRESI-MS. Compounds I and II showed promising α-amylase inhibitory activities (IC50 = 1.23 ± 0.06-4.5 ± 0.03μM) as compared to the standard acarbose (IC50 1.20 ± 0.09μM). In addition to that all derivatives were found good to moderate scavengers of DPPH (IC50 = 2.01 ± 0.13-5.3 ± 0.11) and ABTS (IC50 = 2.34 ± 0.07-5.5 ± 0.07μM) radicals, in comparison with standard ascorbic acid having scavenging activities with IC50 = 1.99 ± 0.09μM and IC50 = 2.03 ± 0.11μM for DPPH and ABTS radicals. In-silico mol. docking study was conducted to rationalized the binding interaction of α-amylase enzyme with ligands. Compounds were observed as mixed type inhibitors in enzyme kinetic characterization.

Bioorganic Chemistry published new progress about Antioxidants. 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Application In Synthesis of 22952-32-5.

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