Month: November 2022

Rafiemanzelat, Fatemeh published the artcileRapid synthesis of new block copolyurethanes derived from L-leucine cyclodipeptide in reusable molten ammonium salts: novel and efficient green media for the synthesis of new hydrolysable and biodegradable copolyurethanes, Safety of N-Benzyl-N,N-dibutylbutan-1-aminium chloride, the publication is Amino Acids (2012), 42(6), 2177-2186, database is CAplus and MEDLINE.

This study concerns the synthesis of novel multi block polyurethane (PU) copolymers containing cyclodipeptide, taking the advantage of ionic liquids (ILs) under microwave irradiation For this, L-leucine anhydride cyclodipeptide (LACP) was prepared and then a new class of poly(ether-urethane-urea)s (PEUUs) was synthesized in molten ammonium type ILs. ILs were used as reaction media and PUs were prepared via two-step polymerization method. In the first step, 4,4′-methylene-bis-(4-phenylisocyanate) (MDI) was reacted with LACP to produce isocyanate-terminated oligo(imide-urea) as hard segment (NCO-OIU). Chain extension of the aforementioned pre-polymer with polyethyleneglycol (PEG) of mol. weights of 1000 (PEG-1000) was the second step to furnish a series of new PEUUs. These multiblock copolymers are thermally stable, soluble in amide-type solvents, hydrolysable and biodegradable. PEUUs prepared in ILs under microwave irradiation showed more phase separation and crystallinity than PEUUs prepared under conventional method. The protocol presented here has the merits of environmentally benign, simple operation, convenient work-up, short reaction time and good yields without using volatile organic solvents, and catalysts. Ammonium type reaction media were air and water stable, and relatively cheap, which makes them suitable for application. The results demonstrate that they can be easily separated into water and reused without losing activity. Reusability of tetrabutylammonium bromide as reaction media makes the method a cost effective and environmentally benign method under microwave irradiation Thus, we could prepare environmentally friendly polymers via environmentally benign method.

Amino Acids published new progress about 23616-79-7. 23616-79-7 belongs to chlorides-buliding-blocks, auxiliary class Phase Transfer Catalyst, name is N-Benzyl-N,N-dibutylbutan-1-aminium chloride, and the molecular formula is C19H34ClN, Safety of N-Benzyl-N,N-dibutylbutan-1-aminium chloride.

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

Sabt, Ahmed published the artcileNovel coumarin-6-sulfonamides as apoptotic anti-proliferative agents: synthesis, in vitro biological evaluation, and QSAR studies, Application of Coumarin-6-sulfonyl chloride, the publication is Journal of Enzyme Inhibition and Medicinal Chemistry (2018), 33(1), 1095-1107, database is CAplus and MEDLINE.

Herein, we report the synthesis of different novel sets of coumarin-6-sulfonamide derivatives bearing different functionalities (4a, b, 8a-d, 11a-d, 13a, b, and 15a-c), and in vitro evaluation of their growth inhibitory activity towards the proliferation of three cancer cell lines; HepG2 (hepatocellular carcinoma), MCF-7 (breast cancer), and Caco-2 (colon cancer). HepG2 cells were the most sensitive cells to the influence of the target coumarins. Compounds and emerged as the most active members against HepG2 cells (IC₅₀ = 3.48 ± 0.28 and 5.03 ± 0.39 μM, resp.). Compounds and were able to induce apoptosis in HepG2 cells, as assured by the upregulation of the Bax and downregulation of the Bcl-2, besides boosting caspase-3 levels. Besides, compound induced a significant increase in the percentage of cells at Pre-G1 by 6.4-folds, with concurrent significant arrest in the G2-M phase by 5.4-folds compared to control. Also, displayed significant increase in the percentage of annexin V-FITC pos. apoptotic cells from 1.75-13.76%. Moreover, QSAR models were established to explore the structural requirements controlling the anti-proliferative activities.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about 10543-42-7. 10543-42-7 belongs to chlorides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Chloride,Sulfonyl chlorides,Ester, name is Coumarin-6-sulfonyl chloride, and the molecular formula is C9H5ClO4S, Application of Coumarin-6-sulfonyl chloride.

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

Milik, Sandra N. published the artcileSurmounting the resistance against EGFR inhibitors through the development of thieno[2,3-d]pyrimidine-based dual EGFR/HER2 inhibitors, Category: chlorides-buliding-blocks, the publication is European Journal of Medicinal Chemistry (2018), 316-336, database is CAplus and MEDLINE.

In light of the emergence of resistance against the currently available EGFR inhibitors, our study focuses on tackling this problem through the development of dual EGFR/HER2 inhibitors with improved enzymic affinities. Guided by the binding mode of the marketed dual EGFR/HER2 inhibitor, Lapatinib, we proposed the design of dual EGFR/HER2 inhibitors based on the 6-phenylthieno[2,3-d]pyrimidine as a core scaffold and hinge binder. After two cycles of screening aiming to identify the optimum aniline headgroup and solubilizing group, we eventually identified 27b as a dual EGFR/HER2 inhibitor with IC₅₀ values of 91.7 nM and 1.2 μM, resp. Notably, 27b dramatically reduced the viability of various patient-derived cancer cells preferentially overexpressing EGFR/HER2 (A431, MDA-MBA-361 and SKBr3 with IC₅₀ values of 1.45, 3.5 and 4.83 μM, resp.). Addnl., 27b efficiently thwarted the proliferation of lapatinib-resistant human non-small lung carcinoma (NCI-H1975) cells, harboring T790 M mutation, with IC₅₀ of 4.2 μM. Consistently, 27b significantly blocked EGF-induced EGFR activation and inactivated its downstream AKT/mTOR/S6 signalling pathway triggering apoptotic cell death in NCI-H1975 cells. The present study presents a promising candidate for further design and development of novel EGFR/HER2 inhibitors capable of overcoming EGFR TKIs resistance.

European Journal of Medicinal Chemistry published new progress about 350-30-1. 350-30-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Nitro Compound,Benzene, name is 3-Chloro-4-fluoronitrobenzene, and the molecular formula is C6H3ClFNO2, Category: chlorides-buliding-blocks.

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

Abdel Bary, Hamed M. published the artcileReaction with coumarin. IV, Synthetic Route of 10543-42-7, the publication is Afinidad (1995), 52(459), 344-6, database is CAplus.

Coumarin-6-sulfonyl chloride (I) reacts with 4-aminobenzenesulfonamide or 2-amino-1,3,4-thiadiazole-5-sulfonamide at the sulfonamido amino group, leaving the amino group attached to the ring unreacted. Reaction of I with 4-aminoacetophenone, or with o-, m-, or p-phenylenediamine, gives corresponding mono- and bis-sulfonamides II or III, resp. II reacts with hydrazine hydrate or phenylhydrazine to yield hydrazones. Ortho-III is cyclized with aldehydes to give benzimidazole derivatives

Afinidad published new progress about 10543-42-7. 10543-42-7 belongs to chlorides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Chloride,Sulfonyl chlorides,Ester, name is Coumarin-6-sulfonyl chloride, and the molecular formula is C9H5ClO4S, Synthetic Route of 10543-42-7.

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

Washburn, Alex published the artcileDual-targeting GroEL/ES chaperonin and protein tyrosine phosphatase B (PtpB) inhibitors: A polypharmacology strategy for treating Mycobacterium tuberculosis infections, Category: chlorides-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry Letters (2019), 29(13), 1665-1672, database is CAplus and MEDLINE.

Benzoxazolylphenyl sulfonamides I (R = Me, Ph, 2-thienyl, 2-FC₆H₄, 3-FC₆H₄, 4-FC₆H₄, 2-ClC₆H₄, 3-ClC₆H₄, 4-ClC₆H₄, 5-chloro-2-thienyl, 2-F₃CC₆H₄, 3-F₃CC₆H₄, 4-F₃CC₆H₄, 3,4-Cl₂C₆H₃, 4-F-3-F₃CC₆H₃, 4-Cl-3-F₃CC₆H₃, 4-Cl-3-O₂NC₆H₃, 5-Cl-2-MeOC₆H₃, 2-MeC₆H₄, 3-MeC₆H₄, 4-MeC₆H₄, 4-EtC₆H₄, 4-H₂C:CHC₆H₄, 2-MeOC₆H₄, 3-MeOC₆H₄, 4-MeOC₆H₄, 2-HOC₆H₄, 3-HOC₆H₄, 4-HOC₆H₄) and phenylbenzoxazolyl sulfonamides II (R = Me, Ph, 2-thienyl, 2-FC₆H₄, 3-FC₆H₄, 4-FC₆H₄, 2-ClC₆H₄, 3-ClC₆H₄, 4-ClC₆H₄, 5-chloro-2-thienyl, 2-F₃CC₆H₄, 3-F₃CC₆H₄, 4-F₃CC₆H₄, 3,4-Cl₂C₆H₃, 4-F-3-F₃CC₆H₃, 4-Cl-3-F₃CC₆H₃, 4-Cl-3-O₂NC₆H₃, 5-Cl-2-MeOC₆H₃, 2-MeC₆H₄, 3-MeC₆H₄, 4-MeC₆H₄, 4-EtC₆H₄, 4-H₂C:CHC₆H₄, 2-MeOC₆H₄, 3-MeOC₆H₄, 4-MeOC₆H₄, 2-HOC₆H₄, 3-HOC₆H₄, 4-HOC₆H₄) were prepared as dual inhibitors of GroEL/ES and the virulence factor protein tyrosine phosphatase B (PtpB) for the treatment of Mycobacterium tuberculosis infection at all stages of bacterial infection.

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 C15H21BO2, Category: chlorides-buliding-blocks.

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

Fawzy, Ahmed published the artcileDegradation of Ampicillin and Flucloxacillin Antibiotics via Oxidation by Alkaline Hexacyanoferrate(III): Kinetics and Mechanistic Aspects, Category: chlorides-buliding-blocks, the publication is Industrial & Engineering Chemistry Research (2020), 59(37), 16217-16224, database is CAplus.

The kinetics and mechanistic aspects of the oxidation of two beta-lactam antibiotics (A), ampicillin and flucloxacillin, by alk. hexacyanoferrate(III) (HCF(III)) were examined using spectrophotometry at a fixed temperature The oxidation reactions showed a 1:4 (A: HCF(III)) stoichiometry. The reaction kinetics were found to follow first-order dependence for the oxidant and fractional first-order dependence for [A] and [OH^–]. The enhancement of the ionic strength and dielec. constant was found to increase the oxidation rates. Free radical tests of the reactions showed pos. results. The addition of HCF(II) as a predicted oxidation product did not considerably change the oxidation rates. Under the same exptl. conditions, the oxidation rate of ampicillin was found to be slightly lower than that of flucloxacillin. The acquired oxidation products were recognized using spot testing and Fourier transform IR spectra. A conceivable oxidation mechanism was suggested. A derived rate law expression was found to be consistent with the exptl. results. The activation parameters were assessed and discussed.

Industrial & Engineering Chemistry Research published new progress about 3919-74-2. 3919-74-2 belongs to chlorides-buliding-blocks, auxiliary class Isoxazole,Fluoride,Chloride,Carboxylic acid,Benzene, name is 3-(2-Chloro-6-fluorophenyl)-5-methylisoxazole-4-carboxylic acid, and the molecular formula is C11H7ClFNO3, Category: chlorides-buliding-blocks.

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

Fawzy, A. published the artcileMechanistic and thermodynamic aspects of oxidative removal of flucloxacillin by different oxidants in an acidic medium, Category: chlorides-buliding-blocks, the publication is Journal of Molecular Liquids (2021), 115160, database is CAplus.

The mechanism of oxidative removal of flucloxacillin antibiotic (Flx) by two different oxidants (Ox), potassium bromate (KBrO3) and potassium iodate (KIO3), were studied using a spectrophotometric technique in sulfuric acid medium. The stoichiometry of the oxidation reactions of flucloxacillin by both oxidants was set to be a 2: 3 (Ox: Flx). The oxidation products of flucloxacillin were identified utilizing spot tests and FT-IR spectroscopy. The reactions followed a first order credence in [Flx] and lesser than unit order kinetics regarding to both [Ox] and [H+]. Negligible impacts of both ionic strength and dielec. constant of the reactions medium on the rates of reactions were observed The dependence of the oxidation rates on mercuric acetate concentration which works as a scavenger for any bromide or iodide ion composed during the reactions was investigated. Credence of reaction rates on temperature was studied, and the activation parameters were assessed and discussed. Tests for free radicals involvement throughout the oxidation reactions were neg. The reactions mechanism was elucidated and the rate law expressions were derived.

Journal of Molecular Liquids published new progress about 3919-74-2. 3919-74-2 belongs to chlorides-buliding-blocks, auxiliary class Isoxazole,Fluoride,Chloride,Carboxylic acid,Benzene, name is 3-(2-Chloro-6-fluorophenyl)-5-methylisoxazole-4-carboxylic acid, and the molecular formula is C11H7ClFNO3, Category: chlorides-buliding-blocks.

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

El-Naggar, A. M. published the artcileSynthesis and antimicrobial activity of some new N-coumarin-6-sulfonyl amino acid and dipeptide derivatives, SDS of cas: 10543-42-7, the publication is Afinidad (1987), 44(411), 431-3, database is CAplus.

Title amino acids I [X = β-Ala, Val, DL-Val, Leu, p-NHC₆H₄CO (p-Aba), m-NHC₆H₄CO (m-Aba), Tyr, etc.] were prepared by sulfonylating the appropriate amino acid with sulfonyl chloride II. I were esterified with MeOH via SOCl₂ to give the corresponding Me esters. Dipeptides III (X-X¹ = β-Ala-DL-Ser, β-Ala-Leu, Pro-Phe, Phe-Val, etc.) were prepared by coupling the appropriate I with H-X¹-OMe.HCl by DCC in THF containing Et₃N. I (X = β-Ala, p-Aba, m-Aba) and the Me esters of I (X = Leu, Pro) were active against a number of microorganisms.

Afinidad published new progress about 10543-42-7. 10543-42-7 belongs to chlorides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Chloride,Sulfonyl chlorides,Ester, name is Coumarin-6-sulfonyl chloride, and the molecular formula is C9H5ClO4S, SDS of cas: 10543-42-7.

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

Amin, Kamelia M. published the artcileSynthesis, antibreast cancer activity and docking study of some novel 4-(benzo [d] thiazol-2-yl) phenyl moiety as CDK2 inhibitors, SDS of cas: 21286-54-4, the publication is International Journal of Pharmacy and Technology (2016), 8(1), 10853-10871, database is CAplus.

Some novel sulfonamides, Schiff’s bases and pyrrole derivatives attached to 4-benzo[d]thiazol-2-yl were prepared Some of the newly synthesized compounds have been evaluated for their potential cytotoxicity against breast cancer cell line (MCF-7) in comparison with doxorubicin; the urea derivative 6a exhibited the highest activity. Mol. docking into CDK2 has been done for lead optimization of the compounds in study as potential CDK2 inhibitors; compound 8b showed the lowest binding score.

International Journal of Pharmacy and Technology published new progress about 21286-54-4. 21286-54-4 belongs to chlorides-buliding-blocks, auxiliary class Chiral,Chloride,Sulfonyl chlorides,Aliphatic cyclic hydrocarbon,Ketone, name is ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride, and the molecular formula is C10H15ClO3S, SDS of cas: 21286-54-4.

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

Abd El-Bary, H. published the artcileReactions with coumarin. II, SDS of cas: 10543-42-7, the publication is Afinidad (1994), 51(452), 311-14, database is CAplus.

Coumarin-6-sulfonyl chloride (I) reacted with o-, m-, and p-phenylenediamines to give the sulfonamides. Ph isocyanate or Ph isothiocyanate reacted with the sulfonamides yielding urea derivatives Condensation of the sulfonamides with acetaldehyde or acetophenone gave imines. Sulfonic acid esters were formed through condensation of I with phenolic derivatives

Afinidad published new progress about 10543-42-7. 10543-42-7 belongs to chlorides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Chloride,Sulfonyl chlorides,Ester, name is Coumarin-6-sulfonyl chloride, and the molecular formula is C9H5ClO4S, SDS of cas: 10543-42-7.

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