Month: December 2022

Munkuev, Aldar A. published the artcileAdamantane-Monoterpenoid Conjugates Linked via Heterocyclic Linkers Enhance the Cytotoxic Effect of Topotecan, Formula: C10H15ClO3S, the publication is Molecules (2022), 27(11), 3374, database is CAplus and MEDLINE.

Inhibiting tyrosyl-DNA phosphodiesterase 1 (TDP1) is a promising strategy for increasing the effectiveness of existing antitumor therapy since it can remove the DNA lesions caused by anticancer drugs, which form covalent complexes with topoisomerase 1 (TOP1). Here, new adamantane-monoterpene conjugates with a 1,2,4-triazole or 1,3,4-thiadiazole linker core were synthesized, where (+)-and (-)-campholenic and (+)-camphor derivatives were used as monoterpene fragments. The campholenic derivatives showed activity against TDP1 at a low micromolar range with IC₅₀ ~5-6μM, whereas camphor-containing compounds were ineffective. Surprisingly, all the compounds synthesized demonstrated a clear synergy with topotecan, a TOP1 poison, regardless of their ability to inhibit TDP1. These findings imply that different pathways of enhancing topotecan toxicity other than the inhibition of TDP1 can be realized.

Molecules 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

Blazhevs’kii, M. E. published the artcileA spectrophotometric assay for kinetic determination of cholinesterase inhibitors using p-phenetidine oxidation, COA of Formula: C38H74Cl2N2O4, the publication is Farmatsevtichnii Zhurnal (Kiev) (2004), 52-58, database is CAplus.

An assay for detecting cholinesterase inhibitors using p-phenetidine oxidation is described. The high-sensitivity spectrophotometric assay is developed for quant. determination of quaternary ammonium salts, phenothiazine derivatives, phosphonous acid derivatives and some alkaloids. In the concentration range of the analyte 6·10^-19-6·10^-5 M the relative error does not exceed ±11%.

Farmatsevtichnii Zhurnal (Kiev) published new progress about 38146-42-8. 38146-42-8 belongs to chlorides-buliding-blocks, auxiliary class Achiral Phase-Transfer Catalysts, name is N1,N10-Bis(2-((2-isopropyl-5-methylcyclohexyl)oxy)-2-oxoethyl)-N1,N1,N10,N10-tetramethyldecane-1,10-diaminium chloride, and the molecular formula is C38H74Cl2N2O4, COA of Formula: C38H74Cl2N2O4.

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

Kleimenov, B. V. published the artcileMechanism of the action of organic substances containing a trichloromethyl group in reducing friction under high-load conditions, Related Products of chlorides-buliding-blocks, the publication is Teoriya Smazochnogo Deistviya i Novye Materialy (1965), 48-52, database is CAplus.

Acids containing the CCl₃ group have high antiwear properties. These properties decrease considerably after replacing the H of the acid by an aliphatic radical or a base. In the presence of HOAc, the critical load is 96 kg., while with Cl₃CCO₂H, it is ≤300 kg. When CCl₃P(O)(OBu)₂ is applied, the critical load is lower than if a simple acid is used. Heating of CCl₃P(O)(OBu)₂ at 160-80° results in elimination of the hydrocarbon radical with formation of butylene, CCl₃P(O)(OBu)OH, and CCl₃P(O)(OH)₂. Heating of CCl₃P(O)(OH)₂ to 325° gives HCl and CO. No free Cl is formed. Two varieties of interaction between the additive and the metal surface occur: chemisorptive saturation of free bonds of the surface atoms of the metal without destroying the crystal lattice linkage, or full chem. linkage of the reagent with the metal atoms which may destroy the crystal lattice linkage. Thus, 2 antagonistic actions occur: the formation of a chem. modified surface and its destruction. The decrease of wear and seizing is achieved by the acceleration of the chem. modification. The presence of the CCl₃ group polarizes the additive mol. and increases the viscosity of chemisorption onto the surface of the metal. At high temperature of the friction zone, the additive undergoes thermal decomposition and formation of (trichloromethyl)phosphonic acids. These acids interact with the metal to form salts and modify the metallic surface. The interaction is an ionic oxidation-reduction and can be represented by the equation Fe + 2H⁺ = Fe⁺⁺ + 2H. The addition of the CCl₃ group increases the H⁺ concentration in the friction zone, which is one of the main reasons for the antiwear properties of compounds containing the CCl₃ group.

Teoriya Smazochnogo Deistviya i Novye Materialy 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 C5H10Cl3O3P, Related Products of chlorides-buliding-blocks.

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

Cid, Jose Maria published the artcileDiscovery of 1,4-Disubstituted 3-Cyano-2-pyridones: A New Class of Positive Allosteric Modulators of the Metabotropic Glutamate 2 Receptor, Category: chlorides-buliding-blocks, the publication is Journal of Medicinal Chemistry (2012), 55(5), 2388-2405, database is CAplus and MEDLINE.

The discovery and characterization of compound 48, a selective and in vivo active mGlu2 receptor pos. allosteric modulator (PAM), are described. A key to the discovery was the rational exploration of the initial HTS hit 13 guided by an overlay model built with reported mGlu2 receptor PAM chemotypes. The initial weak in vitro activity of the hit 13 was quickly improved, although compounds still had suboptimal druglike properties. Subsequent modulation of the physicochem. properties resulted in compounds having a more balanced profile, combining good potency and in vivo pharmacokinetic properties. Final refinement by addressing cardiovascular safety liabilities led to the discovery of compound (I). Besides good potency, selectivity, and ADME properties, I displayed robust in vivo activity in a sleep-wake EEG (sw-EEG) assay consistent with mGlu2 receptor activation, in accordance with previous work from our laboratories

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

Lesuisse, Dominique published the artcileRational design of potent GSK3β inhibitors with selectivity for Cdk1 and Cdk2, SDS of cas: 766549-26-2, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(6), 1985-1989, database is CAplus and MEDLINE.

From an HTS hit, a series of potent and selective aminoindazole inhibitors of GSK3β have been designed based on a Cdk2-homol. model and with the help of several crystal structures of the compounds within Cdk2.

Bioorganic & Medicinal Chemistry Letters published new progress about 766549-26-2. 766549-26-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Phenol,Boronic Acids,Boronic acid and ester, name is 2-Chloro-4-hydroxyphenylboronic acid, and the molecular formula is C6H6BClO3, SDS of cas: 766549-26-2.

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

Wawrzynczak, Agata published the artcileHydrosilylation of n-alkenes and allyl chloride over platinum supported on styrene-divinylbenzene copolymer, Safety of Dichloro(methyl)(octyl)silane, the publication is Catalysis Today (2011), 169(1), 69-74, database is CAplus.

Catalytic performance of styrene-divinylbenzene copolymer-supported platinum catalyst of high crosslinking degree and high surface area was studied in reactions of hydrosilylation of allyl chloride, 1-octene and 1-butene. The catalyst has shown considerably greater stability of catalytic activity than classical active carbon-supported catalyst. In experiments on repeated use of catalysts, the decrease in catalytic activity for hydrosilylation of liquid double bond-containing compounds proceeding in the presence of the copolymer-supported and carbon-supported platinum was considerably smaller in the case of the former catalyst. Bimetallic Pt-Cu catalyst on polymeric support appeared to be considerably less active than monometallic catalyst.

Catalysis Today published new progress about 14799-93-0. 14799-93-0 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is Dichloro(methyl)(octyl)silane, and the molecular formula is C10H20O2, Safety of Dichloro(methyl)(octyl)silane.

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

Alkayal, Nazeeha published the artcileWell-defined polyethylene-based graft terpolymers by combining nitroxide-mediated radical polymerization, polyhomologation and azide/alkyne “click” chemistry, Quality Control of 5034-06-0, the publication is Polymer Chemistry (2016), 7(17), 2986-2991, database is CAplus.

Novel well-defined polyethylene-based graft terpolymers were synthesized via the “grafting onto” strategy by combining nitroxide-mediated radical polymerization (NMP), polyhomologation and copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) “click” chem. Three steps were involved in this approach: (i) synthesis of alkyne-terminated polyethylene-b-poly(ε-caprolactone) (PE-b-PCL-alkyne) block copolymers (branches) by esterification of PE-b-PCL-OH with 4-pentynoic acid; the PE-b-PCL-OH was obtained by polyhomologation of dimethylsulfoxonium methylide to afford PE-OH, followed by ring opening polymerization of ε-caprolactone using PE-OH as a macroinitiator, (ii) synthesis of random copolymers of styrene (St) and 4-chloromethylstyrene (4-CMS) with various CMS contents, by nitroxide-mediated radical copolymerization (NMP), and conversion of chloride to azide groups by reaction with sodium azide (NaN₃) (backbone) and (iii) “click” linking reaction to afford the PE-based graft terpolymers. All intermediates and final products were characterized by high-temperature size exclusion chromatog. (HT-SEC), Fourier transform IR spectroscopy (FTIR), proton NMR spectroscopy (¹H NMR) and differential scanning calorimetry (DSC).

Polymer Chemistry 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, Quality Control of 5034-06-0.

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

Topolski, M. published the artcileChiral carbenoids: their formation and reactions, HPLC of Formula: 866-23-9, the publication is Journal of Organic Chemistry (1993), 58(3), 546-55, database is CAplus.

Carbenoids, generated by metalation or halogen-metal exchange reactions, have been prepared from chiral vinyl and cyclopropyl halides. The reactivity and stereochem. observed in the reaction of these carbenoids has been interpreted as being due to metal-assisted ionization.

Journal of Organic Chemistry 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 C7H8BNO4, HPLC of Formula: 866-23-9.

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

Kemp, Laura R. published the artcileThe transcriptional regulator CprK detects chlorination by combining direct and indirect readout mechanisms, Computed Properties of 33697-81-3, the publication is Philosophical Transactions of the Royal Society, B: Biological Sciences (2013), 368(1616), 20120323/1-20120323/8, database is CAplus and MEDLINE.

The transcriptional regulator CprK controls the expression of the reductive dehalogenase CprA in organohalide-respiring bacteria. Desulfitobacterium hafniense CprA catalyzes the reductive dechlorination of the terminal electron acceptor o-chlorophenol acetic acid, generating the phenol acetic acid product. It has been shown that CprK has ability to distinguish between the chlorinated CprA substrate and the de-halogenated end product, with an estimated an estimated 10⁴-fold difference in affinity. Using a green fluorescent protein GFP_UV-based transcriptional reporter system, we establish that CprK can sense o-chlorophenol acetic acid at the nanomolar level, whereas phenol acetic acid leads to transcriptional activation only when approaching micromolar levels. A structure-activity relationship study, using a range of o-chlorophenol acetic-acid-related compounds and key CprK mutants, combined with pK_a calculations on the effector binding site, suggests that the sensitive detection of chlorination is achieved through a combination of direct and indirect readout mechanisms. Both the phys. presence of the bulky chloride substituent as well as the accompanying electronic effects lowering the inherent phenol pK_a are required for high affinity. Indeed, transcriptional activation by CprK appears strictly dependent on establishing a phenolate-K133 salt bridge interaction, rather than on the presence of a halogen atom per se. As K133 is strictly conserved within the CprK family, our data suggest that physiol. function and future applications in biosensing are probably restricted to phenolic compounds

Philosophical Transactions of the Royal Society, B: Biological Sciences 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, Computed Properties of 33697-81-3.

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

Drake, R. published the artcilePolymethacrylate and polystyrene-based resin-supported Pt catalysts in room temperature, solvent-less, oct-1-ene hydrosilylations using trichlorosilane and methyldichlorosilane, Product Details of C9H20Cl2Si, the publication is Journal of Molecular Catalysis A: Chemical (2001), 177(1), 49-69, database is CAplus.

A first group of methacrylate-based resins have been prepared with different amine ligands each co-ordinating Pt(II). Evaluation of each of these as room temperature catalysts in the solvent-less hydrosilylation of oct-1-ene by trichlorosilane has identified a supported ethylenediamine-derived ligand as providing the most active and stable Pt catalyst. A second group of methacrylate-based resins and third group of styrene-based resins have also been prepared with a variety of morphologies. Each of these was chem. modified to introduce the same ethylenediamine-derived ligand and subsequently Pt(II) coordinated to each of these. Both groups of resin catalysts were evaluated for activity, selectivity, Pt leaching and recyclability in the hydrosilylation of oct-1-ene by trichlorosilane and methyldichlorosilane. Specific samples of resin catalysts have been recycled up to 11 times in successive batch reactions. The styrene-based resins have been shown to be more active than the methacrylate-based ones, almost certainly because as a group they are more hydrophobic. Gel-type morphologies in the support are totally unsuitable and appear to provide severe mass transport limitations. The various macroporous resin based species are very attractive catalysts and the most likely optimum design criteria are discussed.

Journal of Molecular Catalysis A: Chemical published new progress about 14799-93-0. 14799-93-0 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is Dichloro(methyl)(octyl)silane, and the molecular formula is C9H20Cl2Si, Product Details of C9H20Cl2Si.

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