Tag: M.W=150-200

Imhoff, Viviane published the artcileInhibitors of the carrier-mediated influx of auxin in suspension-cultured tobacco cells, Quality Control of 33697-81-3, the publication is Planta (2000), 210(4), 580-588, database is CAplus and MEDLINE.

Active auxin transport in plant cells is catalyzed by two carriers working in opposite directions at the plasma membrane, the influx and efflux carriers. A role for the efflux carrier in polar auxin transport (PAT) in plants has been shown from studies using phytotropins. Phytotropins have been invaluable in demonstrating that PAT is essential to ensure polarized and coordinated growth and to provide plants with the capacity to respond to environmental stimuli. However, the function of the influx carrier at the whole-plant level is unknown. New auxin-transport inhibitors which could be employed to investigate its function were identified. Thirty-five aryl and aryloxyalkylcarboxylic acids were assayed for their ability to perturb the accumulation of 2,4-D and 1-NAA in suspension-cultured tobacco (Nicotiana tabacum L.) cells. As 2,4-D and 1-NAA are preferentially transported by the influx and efflux carriers, resp., accumulation experiments utilizing synthetic auxins provide independent information on the activities of both carriers. The majority (60%) of compounds half-inhibited the carrier-mediated influx of [¹⁴C]2,4-D at concentrations of less than 10 μM. Most failed to interfere with [³H]NAA efflux, at least in the short term. Even though they increasingly perturbed auxin efflux when given a prolonged treatment, several compounds were much better at discriminating between influx and efflux carrier activities than naphthalene-2-acetic acid which is commonly employed to investigate influx-carrier properties. Structure-activity relationships and factors influencing ligand specificity with regard to auxin carriers are discussed.

Planta 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, Quality Control of 33697-81-3.

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

Takahashi, Hidehiko published the artcileChemical aspects of plateau formation in the action current of the myelinated nerve fiber, Product Details of C7H16ClNO2, the publication is Japan. J. Physiol. (1960), 280-91, database is CAplus.

Among simple oxidizing agents, only H₂O₂ at concentrations higher than 2% produced a plateau in toad single myelinated nerve fibers in the temporal course of action current. Its effect was mainly due to hypertonicity, but its oxidizing potency was somewhat favorable to plateau formation. p-Quinone depolarized the Ranvier’s node and delayed the repolarization phase at the same time. Although recovery with the addition of cysteine was not so good, its effect was essentially attributable to its oxidizing potency, for hydroquinone at high concentrations caused deterioration. In the plasma membrane of the Ranvier’s node, the repolarization phase of action potential can be delayed most effectively by the –S–M–S– linkage (M represents bivalent transition metals).

Japan. J. Physiol. published new progress about 6249-56-5. 6249-56-5 belongs to chlorides-buliding-blocks, auxiliary class Phase Transfer Catalyst,Inhibitor,Natural product, name is 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride, and the molecular formula is C6H8N2, Product Details of C7H16ClNO2.

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

Jagadeesh, Rajenahally V. published the artcileMOF-derived cobalt nanoparticles catalyze a general synthesis of amines, Product Details of C6H3ClFNO2, the publication is Science (Washington, DC, United States) (2017), 358(6361), 326-332, database is CAplus and MEDLINE.

The development of base metal catalysts for the synthesis of pharmaceutically relevant compounds remains an important goal of chem. research. Here, we report that cobalt nanoparticles encapsulated by a graphitic shell are broadly effective reductive amination catalysts. Their convenient and practical preparation entailed template assembly of cobalt-diamine-dicarboxylic acid metal organic frameworks on carbon and subsequent pyrolysis under inert atm. The resulting stable and reusable catalysts were active for synthesis of primary, secondary, tertiary, and N-methylamines (more than 140 examples). The reaction couples easily accessible carbonyl compounds (aldehydes and ketones) with ammonia, amines, or nitro compounds, and mol. hydrogen under industrially viable and scalable conditions, offering cost-effective access to numerous amines, amino acid derivatives, and more complex drug targets.

Science (Washington, DC, United States) 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, Product Details of C6H3ClFNO2.

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

Senthamarai, Thirusangumurugan published the artcileExpedient Synthesis of N-Methyl- and N-Alkylamines by Reductive Amination using Reusable Cobalt Oxide Nanoparticles, Safety of 3-Chloro-4-fluoronitrobenzene, the publication is ChemCatChem (2018), 10(6), 1235-1240, database is CAplus.

N-Methyl- and N-alkylamines represent important fine and bulk chems. that are extensively used in both academic research and industrial production Notably, these structural motifs are found in a large number of life-science mols. and play vital roles in regulating their activities. Therefore, the development of convenient and cost-effective methods for the synthesis and functionalization of amines by using earth-abundant metal-based catalysts is of scientific interest. In this regard, an expedient reductive amination process for the selective synthesis of N-methylated and N-alkylated amines by using nitrogen-doped, graphene-activated nanoscale Co₃O₄-based catalysts, is reported. Starting from inexpensive and easily accessible nitroarenes or amines and aqueous formaldehyde or aldehydes in the presence of formic acid, this cost-efficient reductive amination protocol allows the synthesis of various N-methyl- and N-alkylamines, amino acid derivatives, and existing drug mols.

ChemCatChem 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 C9H9F5Si, Safety of 3-Chloro-4-fluoronitrobenzene.

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

Wan, Zhongliang published the artcileSynthesis and Biological Activity of 3-N-Substituted Estrogen Derivatives as Breast Cancer Agents, Product Details of C5H13Cl2N, the publication is Mini-Reviews in Medicinal Chemistry (2013), 13(9), 1381-1388, database is CAplus and MEDLINE.

3-N-substituted-estrogen derivatives I [R = 3-morpholinopropyl, (CH₂)₃NMe₂, CH(Me)CH₂NMe₂, 3-piperidinopropyl, 3-aminopropyl, etc.] were synthesized and characterized. Their antiproliferative activities against human ER(+) MCF-7 (breast), ER(-) MDA-MB-231 (breast) and Ishikawa (endometrial) cancer cell lines were determined after 72 h drug exposure employing CellTiter-Glo assay at concentrations ranging from (0.01-100,000 nM). The antiproliferative activities of these compounds were compared to tamoxifen (TAM), 4-hydroxytamoxifen (4-OHT, active metabolite of tamoxifen) and raloxifene (RAL). In vitro results indicated that compound I (R = 3-piperidinopropyl) (IC₅₀ = 12μM) displayed comparable antiproliferative activity against MDA-MB 231 cell line; while compounds I [R = (CH₂)₃NMe₂, CH(Me)CH₂NMe₂, (CH₃)₃NEt₂] (IC₅₀ = 12μM) displayed higher activity against MCF-7 and Ishikawa cell lines, in comparison to TAM activity (19-33μM).

Mini-Reviews in Medicinal Chemistry published new progress about 4584-49-0. 4584-49-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Salt,Amine,Aliphatic hydrocarbon chain, name is 2-Chloro-N,N-dimethylpropan-1-amine hydrochloride, and the molecular formula is C13H17BrO3, Product Details of C5H13Cl2N.

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

Wagh, Ravindra B. published the artcileSilica chloride: An efficient promoter for oxidation of arylboronic acids to phenols, Quality Control of 209919-30-2, the publication is Tetrahedron Letters (2017), 58(33), 3323-3326, database is CAplus.

This work reports simple, highly efficient protocol for the oxidation of arylboronic acids. Various arylboronic acids were selectively and completely converted into their corresponding oxidized phenols using H₂O₂ as an oxidant in presence of catalytic amount of silica chloride. The results show that silica chloride is a suitable and efficient promoter for the oxidation of arylboronic acids. Heterogeneous catalyst, mild reaction conditions, easy availability of the reagent, easy work-up, excellent yield of corresponding phenols, short reaction time and broad substrate scope makes this protocol attractive and a practical alternative to the existing methods.

Tetrahedron Letters 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 C7H8FNO2S, Quality Control of 209919-30-2.

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

Dyrager, Christine published the artcileDesign, Synthesis, and Biological Evaluation of Chromone-Based p38 MAP Kinase Inhibitors, Category: chlorides-buliding-blocks, the publication is Journal of Medicinal Chemistry (2011), 54(20), 7427-7431, database is CAplus and MEDLINE.

3-(4-Fluorophenyl)-2-(4-pyridyl)chromone derivatives were synthesized and evaluated as p38 MAP kinase inhibitors. Introduction of an amino group in the 2-position of the pyridyl moiety gave p38α inhibitors with IC₅₀ in the low nanomolar range. For instance, 3-(4-fluorophenyl)-2-[-2-(isopropylamino)-4-pyridinyl]chromone (I) has IC₅₀ of 17 nm. I and its cyclohexylamino counterpart showed excellent selectivity profiles when tested on a panel of 62 kinases, as well as efficient inhibition of p38 signaling in human breast cancer cells.

Journal of Medicinal Chemistry published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Category: chlorides-buliding-blocks.

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

Hoejer Holmgren, Karin published the artcileRoute Determination of Sulfur Mustard Using Nontargeted Chemical Attribution Signature Screening, Safety of 1,2-Bis(2-chloroethyl)disulfane, the publication is Analytical Chemistry (Washington, DC, United States) (2021), 93(11), 4850-4858, database is CAplus and MEDLINE.

Route determination of sulfur mustard was accomplished through comprehensive nontargeted screening of chem. attribution signatures. Sulfur mustard samples prepared via 11 different synthetic routes were analyzed using gas chromatog./high-resolution mass spectrometry. A large number of compounds were detected, and multivariate data anal. of the mass spectrometric results enabled the discovery of route-specific signature profiles. The performance of two supervised machine learning algorithms for retrospective synthetic route attribution, orthogonal partial least squares discriminant anal. (OPLS-DA) and random forest (RF), were compared using external test sets. Complete classification accuracy was achieved for test set samples (2/2 and 9/9) by using classification models to resolve the one-step routes starting from ethylene and the thiodiglycol chlorination methods used in the two-step routes. Retrospective determination of initial thiodiglycol synthesis methods in sulfur mustard samples, following chlorination, was more difficult. Nevertheless, the large number of markers detected using the nontargeted methodol. enabled correct assignment of 5/9 test set samples using OPLS-DA and 8/9 using RF. RF was also used to construct an 11-class model with a total classification accuracy of 10/11. The developed methods were further evaluated by classifying sulfur mustard spiked into soil and textile matrix samples. Due to matrix effects and the low spiking level (0.05% weight/weight), route determination was more challenging in these cases. Nevertheless, acceptable classification performance was achieved during external test set validation: chlorination methods were correctly classified for 12/18 and 11/15 in spiked soil and textile samples, resp.

Analytical Chemistry (Washington, DC, United States) published new progress about 1002-41-1. 1002-41-1 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is 1,2-Bis(2-chloroethyl)disulfane, and the molecular formula is C4H8Cl2S2, Safety of 1,2-Bis(2-chloroethyl)disulfane.

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

Khayyat, Ahdab N. published the artcileDesign, Synthesis, and Antipoliferative Activities of Novel Substituted Imidazole-Thione Linked Benzotriazole Derivatives, Application In Synthesis of 3696-23-9, the publication is Molecules (2021), 26(19), 5983, database is CAplus and MEDLINE.

A new series of benzotriazole moiety bearing substituted imidazol-2-thiones I [R = H, 4-Me, 2-F, etc.] at N1 was designed, synthesized and evaluated for in vitro anticancer activity against the different cancer cell lines MCF-7(breast cancer), HL-60 (Human promyelocytic leukemia), and HCT-116 (colon cancer). Most of the benzotriazole analogs exhibited promising antiproliferative activity against tested cancer cell lines. Among all the synthesized compounds, I [R = 2,4-di-Cl] showed potent activity against the cancer cell lines such as MCF-7, HL-60 and HCT-116 with IC₅₀ 3.57, 0.40 and 2.63μM, resp. Compound I [R = 2,4-di-Cl] was taken up for elaborate biol. studies and the HL-60 cells in the cell cycle were arrested in G2/M phase. Compound I [R = 2,4-di-Cl] showed remarkable inhibition of tubulin polymerization with the colchicine binding site of tubulin. In addition, compound I [R = 2,4-di-Cl] promoted apoptosis by regulating the expression of pro-apoptotic protein BAX and anti-apoptotic proteins Bcl-2. These results provide guidance for further rational development of potent tubulin polymerization inhibitors for the treatment of cancer.

Molecules published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C7H7ClN2S, Application In Synthesis of 3696-23-9.

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

Ahdenov, Reza published the artcileEelectrosynthesis of benzothiazole derivatives via C-H thiolation, Synthetic Route of 3696-23-9, the publication is Heterocyclic Communications (2022), 28(1), 67-74, database is CAplus.

Benzothiazole derivatives are essential intermediates in synthesizing a wide variety of medical and pharmaceutical compounds, and there is a great demand for a simple and efficient method to synthesize benzothiazoles under mild reaction conditions. Organic electrosynthesis as an energy-efficient process represents an environmentally benign and safer method than traditional methods for organic synthesis. Herein, authors present bromine-free and straightforward synthesis of 2-amino benzothiazole derivatives via the reaction of aniline derivatives and ammonium thiocyanate using electrosynthesis in the presence of sodium bromide both as an electrolyte and as a brominating agent at room temperature in iso-Pr alc. (i-PrOH) as a solvent. The reaction of ammonium thiocyanate via C-H thiolation routes, using various aniline derivatives, resulted in a simple, green, and bromine-free synthesis of 2-amino benzothiazole in moderate to good yields under mild reaction conditions. Riluzole drug can be produced using the same procedure in moderate yields.

Heterocyclic Communications published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C7H7ClN2S, Synthetic Route of 3696-23-9.

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