Month: December 2022

Anchordoguy, Thomas J. published the artcileInsights into the cryoprotective mechanism of dimethyl sulfoxide for phospholipid bilayers, Name: trimethyloxosulphonium chloride, the publication is Cryobiology (1991), 28(5), 467-23, database is CAplus and MEDLINE.

DMSO is a widely used cryoprotectant for biol. structures such as membranes. Despite hundreds of studies on the effects of this mol., surprisingly little is known about its cryoprotective mechanism. This study investigates the ability of various DMSO analogs to serve as cryoprotectants for liposomes. The data show that an increase in hydrophobicity progressively reduces the cryoprotective effect of sulfoxides. Addnl. experiments using phospholipid vesicles of varying composition demonstrate that DMSO is markedly less effective on liposomes carrying a net neg. charge. In fact, cryoprotection by DMSO was virtually eliminated in vesicles composed of 30% phosphatidylserine (a neg. charged lipid). Based on these results, it is suggested that the polar sulfoxide moiety of DMSO interacts electrostatically with phospholipid membranes and that this interaction is critical for DMSO’s cryoprotective effect for membranes.

Cryobiology published new progress about 5034-06-0. 5034-06-0 belongs to chlorides-buliding-blocks, auxiliary class Salt,Aliphatic hydrocarbon chain, name is trimethyloxosulphonium chloride, and the molecular formula is C3H9ClOS, Name: trimethyloxosulphonium chloride.

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

Lumeras, Wenceslao published the artcileDesign, Synthesis, and Structure-Activity Relationships of Aminopyridine N-Oxides, a Novel Scaffold for the Potent and Selective Inhibition of p38 Mitogen Activated Protein Kinase, Synthetic Route of 209919-30-2, the publication is Journal of Medicinal Chemistry (2009), 52(17), 5531-5545, database is CAplus and MEDLINE.

A novel series of aminopyridine N-oxides, e.g. I, were designed, synthesized, and tested for their ability to inhibit p38α MAP kinase. Some of these compounds showed a significant reduction in the LPS-induced TNFα production in human whole blood. Structure-activity relationship studies revealed that N-oxide oxygen was essential for activity and was probably a determinant factor for a marked selectivity against other related kinases. Compound I was identified as a potent and selective p38α inhibitor with an appropriate balance between potency and pharmacokinetics. In vivo efficacy of I was demonstrated in reducing TNFα levels in an acute murine model of inflammation (ED₅₀ = 1 mg/kg in LPS-induced TNFα production when dosed orally 1.5 h prior to LPS administration). The oral efficacy of I was further demonstrated in a chronic model of adjuvant arthritis in rats with established disease when administered orally (ED₅₀ = 4.5 mg/kg).

Journal of Medicinal Chemistry published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Synthetic Route of 209919-30-2.

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

Pla-Lopez, Alberto published the artcileSynthesis and Biological Evaluation of Small Molecules as Potential Anticancer Multitarget Agents, Quality Control of 620-20-2, the publication is International Journal of Molecular Sciences (2022), 23(13), 7049, database is CAplus and MEDLINE.

Twenty-six triazole-based derivatives were designed for targeting both PD-L1 (programmed death receptor ligand 1) and VEGFR-2 (vascular endothelial growth factor receptor 2). These compounds were synthesized and biol. evaluated as multitarget inhibitors of VEGFR-2, PD-L1 and c-Myc proteins. The antiproliferative activity of these mols. on several tumor cell lines (HT-29, A-549, and MCF-7) and on the non-tumor cell line HEK-293 was determined The effects on the abovementioned biol. targets were evaluated for some selected compounds Compound I, bearing a p-chlorophenyl group, showed better results than sorafenib in regard to the downregulation of VEGFR-2 and a similar effect to BMS-8 on both PD-L1 and c-Myc proteins. The antiangiogenic and antivascular activities of chloro derivatives were also established by endothelial microtube formation assay on Matrigel.

International Journal of Molecular Sciences published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C7H6Cl2, Quality Control of 620-20-2.

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

Rodriguez-Ortega, Pilar G. published the artcileSynthesis and Structural Characterization of a Ubiquitous Transformation Product (BTS 40348) of Fungicide Prochloraz, COA of Formula: C11H14Cl3NO, the publication is Journal of Agricultural and Food Chemistry (2019), 67(31), 8641-8648, database is CAplus and MEDLINE.

Prochloraz is a widely used imidazole fungicide that has to be analyzed together with its metabolites or transformation products for food safety monitoring purposes in the European Union. Although the focus in food of plant origin has been set on metabolites BTS 44595 and BTS 44596, we consider relevant the study of BTS 40348 metabolite, too, because it has been detected in both raw and processed foods based on citrus fruits in the EU. Metabolite BTS 40348 should be monitored in surface water due to its ecotoxicol. effects. In this work, the synthesis and structural characterization of BTS 40348 metabolite of fungicide prochloraz is presented, because the structure is closely related to the chem. and biol. activity of the substance. Characterization using ¹³C and ¹H NMR, IR, and Raman spectroscopy is detailed, together with confirmation by electrospray mass spectrometry anal.

Journal of Agricultural and Food Chemistry published new progress about 67747-01-7. 67747-01-7 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Ether,Benzene Compounds, name is N-(2-(2,4,6-Trichlorophenoxy)ethyl)propan-1-amine, and the molecular formula is C11H14Cl3NO, COA of Formula: C11H14Cl3NO.

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

Nuti, Elisa published the artcileN-O-Isopropyl Sulfonamido-Based Hydroxamates: Design, Synthesis and Biological Evaluation of Selective Matrix Metalloproteinase-13 Inhibitors as Potential Therapeutic Agents for Osteoarthritis, Formula: C13H12BClO3, the publication is Journal of Medicinal Chemistry (2009), 52(15), 4757-4773, database is CAplus and MEDLINE.

The synthesis and in vitro evaluation of a new series of selective matrix metalloproteinase-13 (MMP-13) inhibitors possessing an arylsulfonamidic scaffold was reported. Among these potential inhibitors, I was discovered exhibiting nanomolar activity for MMP-13 and was highly selective for this enzyme compared to MMP-1, -14, and TACE. Compound I acted as a slow-binding inhibitor of MMP-13 and was demonstrated to be effective in an in vitro collagen assay and in a model of cartilage degradation Furthermore, a docking study was conducted for this compound in order to investigate its binding interactions with MMP-13 and the reasons for its selectivity toward MMP-13 vs. other MMPs.

Journal of Medicinal Chemistry published new progress about 870778-91-9. 870778-91-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (4-((4-Chlorobenzyl)oxy)phenyl)boronic acid, and the molecular formula is C13H12BClO3, Formula: C13H12BClO3.

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

Abrams, Rachel P. published the artcileFive-Membered Ring Peroxide Selectively Initiates Ferroptosis in Cancer Cells, Formula: C10H15ClO3S, the publication is ACS Chemical Biology (2016), 11(5), 1305-1312, database is CAplus and MEDLINE.

A 1,2-dioxolane (FINO₂) was identified as a lead compound from a screen of organic peroxides. FINO₂ does not induce apoptosis, but instead initiates ferroptosis, an iron-dependent, oxidative cell death pathway. Few compounds are known to induce primarily ferroptosis. In contrast to the perceived instability of peroxides, FINO₂ was found to be thermally stable to at least 150 °C. FINO₂ was more potent in cancer cells than nonmalignant cells of the same type. One of the enantiomers was found to be more responsible for the observed activity.

ACS Chemical Biology 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, Formula: C10H15ClO3S.

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

Pierens, Gregory K. published the artcileDetermination of analyte concentration using the residual solvent resonance in ¹H NMR spectroscopy, Category: chlorides-buliding-blocks, the publication is Journal of Natural Products (2008), 71(5), 810-813, database is CAplus and MEDLINE.

An NMR protocol that uses the residual proton signal from DMSO-d₆ (i.e., DMSO-d₅) to determine the concentration of an analyte in a NMR sample was developed. This technique provides an alternative method for determining the molar concentration of compounds in solution without prior knowledge of their mol. weight The method is particularly useful when submilligram quantities of compound are to be analyzed and is applicable to a variety of different research areas such as compound management, and natural product, combinatorial, and medicinal chem.

Journal of Natural Products published new progress about 33697-81-3. 33697-81-3 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Phenol, name is 3-Chloro-4-hydroxyphenylacetic acid, and the molecular formula is C8H7ClO3, Category: chlorides-buliding-blocks.

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

Waschbusch, Rachel published the artcileA new route to α-fluorovinylphosphonates utilizing Peterson olefination methodology, Formula: C5H10Cl3O3P, the publication is Tetrahedron (1996), 52(45), 14199-14216, database is CAplus.

Several α-fluorovinylphosphonates were synthesized from the Peterson olefination reaction applied to both aldehydes and ketones in conjunction with α-lithiated-α-fluoro-α-trimethylsilymethylphosphonate. The reaction with aldehydes gives mainly the E-isomer whereas reaction with ketones gives mainly the Z-isomer. The authors propose a closed transition state to explain the results.

Tetrahedron published new progress about 866-23-9. 866-23-9 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is Diethyltrichloromethylphosphonate, and the molecular formula is C15H18BF3O2, Formula: C5H10Cl3O3P.

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

Anchordoguy, Thomas J. published the artcileEffects of protein perturbants on phospholipid bilayers, Synthetic Route of 5034-06-0, the publication is Archives of Biochemistry and Biophysics (1990), 283(2), 356-61, database is CAplus and MEDLINE.

Series of alcs., amides, ureas, and sulfoxides with increasingly longer hydrocarbon chains lower progressively the thermal denaturation temperature of proteins. Several classes of compounds were investigated for effects on the stability of phospholipid vesicles. Many compounds that are known to perturb protein function also destabilize phospholipid bilayers as reflected by solute-induced loss of vesicle contents.

Archives of Biochemistry and Biophysics published new progress about 5034-06-0. 5034-06-0 belongs to chlorides-buliding-blocks, auxiliary class Salt,Aliphatic hydrocarbon chain, name is trimethyloxosulphonium chloride, and the molecular formula is C3H9ClOS, Synthetic Route of 5034-06-0.

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

Warford, C. Chad published the artcileFrom slow to fast – the user controls the rate of the release of molecules from masked forms using a photoswitch and different types of light, Application In Synthesis of 219537-97-0, the publication is Chemical Communications (Cambridge, United Kingdom) (2015), 51(32), 7039-7042, database is CAplus and MEDLINE.

Exposure to UV light generates a ring-closed isomer of a diarylethene, which undergoes very slow bond breaking and release even after the light is turned off. The rate of release is increased by exposing the isomer to UV and/or visible light.

Chemical Communications (Cambridge, United Kingdom) published new progress about 219537-97-0. 219537-97-0 belongs to chlorides-buliding-blocks, auxiliary class Fused/Partially Saturated Cycles,Cyclopentenes, name is 5-Chloro-3-[2-(5-chloro-2-methylthien-3-yl)cyclopent-1-en-1-yl]-2-methylthiophene, and the molecular formula is C8H11BO2, Application In Synthesis of 219537-97-0.

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