Category: 32333-53-2

Yang, Shichao published the artcileVisible-Light Photoredox-Catalyzed Regioselective Sulfonylation of Alkenes Assisted by Oximes via [1,5]-H Migration, Computed Properties of 32333-53-2, the publication is Journal of Organic Chemistry (2020), 85(2), 564-573, database is CAplus and MEDLINE.

Herein, a visible-light photoredox-catalyzed regioselective sulfonylation of alkenes with sulfonyl hydrazides assisted by oximes at room temperature, which affords a variety of sulfones in good yields is reported. The initial mechanistic experiments demonstrate that the hydroxyl group within oximes plays a crucial role in this sulfonylation.

Journal of Organic Chemistry published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C5H10O, Computed Properties of 32333-53-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Fu, Ying published the artcileA visible-light photoinduced charge-transfer complex promoted the ring opening of N-alkyl-4-piperidinols, Safety of 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, the publication is Green Chemistry (2020), 22(7), 2264-2269, database is CAplus.

A visible-light photoinduced ring opening of N-alkyl-4-piperidinols under mild conditions was achieved. The reaction sequence involved a visible-light-induced charge-transfer complex, which promoted the S-Cl bond cleavage of sulfonyl chlorides. The generated sulfonyl radical further reacts with N-alkyl-4-piperidinol cation radicals to achieve C-N and C-C bond cleavages to yield homoallylamine products.

Green Chemistry published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, Safety of 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Sonoshita, Masahiro published the artcileA whole-animal platform to advance a clinical kinase inhibitor into new disease space, Quality Control of 32333-53-2, the publication is Nature Chemical Biology (2018), 14(3), 291-298, database is CAplus and MEDLINE.

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.

Nature Chemical Biology published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C8H10S, Quality Control of 32333-53-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Abdeen, Sanofar published the artcileSulfonamido-2-arylbenzoxazole GroEL/ES Inhibitors as Potent Antibacterials against Methicillin-Resistant Staphylococcus aureus (MRSA), Recommanded Product: 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, the publication is Journal of Medicinal Chemistry (2018), 61(16), 7345-7357, database is CAplus and MEDLINE.

Extending from a study we recently published examining the anti-trypanosomal effects of a series of GroEL/ES inhibitors based on a pseudo-sym. bis-sulfonamido-2-phenylbenzoxazole scaffold, here, we report the antibiotic effects of asym. analogs of this scaffold against a panel of bacteria known as the ESKAPE pathogens (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter species). While GroEL/ES inhibitors were largely ineffective against K. pneumoniae, A. baumannii, P. aeruginosa, and E. cloacae (Gram-neg. bacteria), many analogs were potent inhibitors of E. faecium and S. aureus proliferation (Gram-pos. bacteria – EC₅₀ values of the most potent analogs were in the 1-2 μM range). Furthermore, even though some compounds inhibit human HSP60/10 biochem. functions in vitro (IC₅₀ values in the 1-10 μM range), many of these exhibited moderate to low cytotoxicity to human liver and kidney cells (CC₅₀ values >20 μM).

Journal of Medicinal Chemistry published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, Recommanded Product: 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Nadirova, Maryana A. published the artcileCascade of the Hinsberg / IMDAF reactions in the synthesis 2-arylsulfonyl-3a,6-epoxyisoindoles and 4a,7-epoxyisoquinolines in water, Name: 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, the publication is Tetrahedron (2021), 132032, database is CAplus.

N-Furfuryl allylamines, readily accessible from corresponding furfurals or furfuryl amines, react with a broad range of aryl sulfonyl chlorides with the formation of a 3a,6-epoxyisoindoles I [Ar = Ph, 2-thienyl, Ts, etc.; R¹ = H, I, Et, etc.; R² = H, Br, Me] in one synthetic stage was reported. Usually, in boiling water, the interaction sequence involved two consecutive steps: the Hinsberg reaction and the intramol. Diels-Alder furane (IMDAF) reaction. The scope and limitations of the proposed method were thoroughly investigated, and it was revealed that the key [4+2] cycloaddition step proceeded through an exo-transition state, giving rise to the exclusive formation of a single diastereomer of the target heterocycle. The method allowed the ability to obtain N-sulfaryl-substituted 3a,6-epoxyisoindoles I and 4a,7-epoxyisoquinolines, which were potentially useful substrates for further transformations and subsequent bioscreening, in particular antimicrobial activity.

Tetrahedron published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, Name: 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Zaib, Sumera published the artcileEvaluation of indole-picolinamide hybrid molecules as carbonic anhydrase-II inhibitors: Biological and computational studies, HPLC of Formula: 32333-53-2, the publication is Journal of Molecular Structure (2022), 133048, database is CAplus.

The present study reported the successful synthesis and evaluation of a series of indole-picolinamide hybrids I, II [Ar = Ph, 3-CF₃C₆H₄, 3,4-di-ClC₆H₃], III, IV and V as potent inhibitors of bovine carbonic anhydrase II, a promising therapeutic target for the treatment of neurol. disorders, osteoporosis, glaucoma, cancer and obesity. Various multistep synthetic approaches were utilized to access the desired structures having exclusive sites for chem. modifications and diverse spots for biol. interactions between the ligand and enzyme. Compound I was observed as a potent inhibitor of the bovine CA-II with an IC₅₀ value of 0.0440 ± 0.009μM. The inhibition potency was about 22-fold higher than the standard drug acetazolamide (IC₅₀ = 0.9618 ± 0.180μM). Several relevant structure-activity relationships were deduced that enlighten the crucial role of substituents as well as the key pharmacophores involved in the inhibition process. Mol. docking tools reinforced the in vitro assay results. The most active compound I was also investigated for anticancer potential using sulforhodamine B assay and results showed two-fold efficacy against HeLa cells when compared to standard drug cisplatin (IC₅₀ = 8.045 ± 3.791μg/mL and 4.128 ± 1.473μg/mL, resp.). These findings were also confirmed by flow cytometry and comet tests. Moreover, fluorescence microscopy with DAPI staining revealed apoptosis as a mechanism of cancer cell death.

Journal of Molecular Structure published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3ClINS, HPLC of Formula: 32333-53-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Kalindjian, S. Barret published the artcileA New Series of Orally Bioavailable Chemokine Receptor 9 (CCR9) Antagonists; Possible Agents for the Treatment of Inflammatory Bowel Disease, HPLC of Formula: 32333-53-2, the publication is Journal of Medicinal Chemistry (2016), 59(7), 3098-3111, database is CAplus and MEDLINE.

Chemokine receptor 9 (CCR9), a cell surface chemokine receptor which belongs to the G protein-coupled receptor, 7-trans-membrane superfamily, is expressed on lymphocytes in the circulation and is the key chemokine receptor that enables these cells to target the intestine. It has been proposed that CCR9 antagonism represents a means to prevent the aberrant immune response of inflammatory bowel disease in a localized and disease specific manner and one which is accessible to small mol. approaches. One possible reason why clin. studies with vercirnon, a prototype CCR9 antagonist, were not successful may be due to a relatively poor pharmacokinetic (PK) profile for the mol. We wish to describe work aimed at producing new, orally active CCR9 antagonists based on the 1,3-dioxoisoindoline skeleton. This study led to a number of compounds that were potent in the nanomolar range and which, on optimization, resulted in several possible preclin. development candidates with excellent PK properties.

Journal of Medicinal Chemistry published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, HPLC of Formula: 32333-53-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Ma, Jia published the artcileDiscovery of novel indole and indoline derivatives against Candida albicans as potent antifungal agents, Safety of 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, the publication is Bioorganic & Medicinal Chemistry Letters (2022), 128826, database is CAplus and MEDLINE.

With the widespread use of azole antifungals in the clinic, the drug resistance has been emerging continuously. In this work, we have designed and prepared a series of novel indole and indoline derivatives, and in vitro antifungal activity against C. albicans were evaluated. The results showed that title compounds exhibited good antifungal effect on Azole-resistant C. albicans. Further mechanism study demonstrated that S18 could inhibit the biofilm formation and hyphae growth of C. albicans through the Ras-cAMP-PKA signaling pathway.

Bioorganic & Medicinal Chemistry Letters published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, Safety of 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Huang, Ke published the artcileSynthesis and biological evaluation of anthraquinone derivatives as allosteric phosphoglycerate mutase 1 inhibitors for cancer treatment, SDS of cas: 32333-53-2, the publication is European Journal of Medicinal Chemistry (2019), 45-57, database is CAplus and MEDLINE.

Phosphoglycerate mutase 1 (PGAM1) coordinates glycolysis, pentose phosphate pathway, and serine synthesis to promote tumor growth through the regulation of its substrate 3-phosphoglycerate (3 PG) and product 2-phosphoglycerate (2 PG). Herein, based on our previously reported PGAM1 inhibitor PGMI-004A, we have developed anthraquinone derivatives as novel allosteric PGAM1 inhibitors and the structure-activity relationship (SAR) was investigated. In addition, we determined the co-crystal structure of PGAM1 and the inhibitor 8g, demonstrating that the inhibitor was located at a novel allosteric site. Among the derivatives, compound 8t was selected for further study, with IC₅₀ values of 0.25 and approx. 5 μM in enzymic and cell-based assays, resp. Mechanistically, compound 8t reduced the glycolysis and oxygen consumption rate in cancer cells, which led to decreased ATP (ATP) production and subsequent 5′ adenosine monophosphate-activated protein kinase (AMPK) activation. The inhibitor 8t also exhibited good efficacy in delaying tumor growth in H1299 xenograft model without obvious toxicity. Taken together, this proof-of-principle work further validates PGAM1 as a potential target for cancer therapy and provides useful information on anti-tumor drug discovery targeting PGAM1.

European Journal of Medicinal Chemistry published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, SDS of cas: 32333-53-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Burns, Mark R. published the artcileStructural correlation between lipophilicity and lipopolysaccharide-sequestering activity in spermine-sulfonamide analogs, Related Products of chlorides-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry Letters (2006), 16(24), 6209-6212, database is CAplus and MEDLINE.

Lipopolysaccharides (LPS), otherwise termed endotoxins, are outer-membrane constituents of Gram-neg. bacteria, and play a key role in the pathogenesis of Septic Shock, a major cause of mortality in the critically ill patient. We had previously defined the pharmacophore necessary for small mols. to specifically bind and neutralize this complex carbohydrate. A series of aryl and aliphatic spermine-sulfonamide analogs were synthesized and tested in a series of binding and cell-based assays in order to probe the effect of lipophilicity on sequestration ability. A strong correlation was indeed found, supporting the hypothesis that endotoxin-neutralizing ability involves a lipophilic or membrane attachment event. The research discussed herein may be useful for the design of addnl. carbohydrate recognizing mols. and endotoxin-neutralizing drugs.

Bioorganic & Medicinal Chemistry Letters published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, Related Products of chlorides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics