Author: Jessica.F

Xu, Shengtao published the artcileA Novel Potent Anticancer Compound Optimized from a Natural Oridonin Scaffold Induces Apoptosis and Cell Cycle Arrest through the Mitochondrial Pathway, Application In Synthesis of 6313-54-8, the publication is Journal of Medicinal Chemistry (2017), 60(4), 1449-1468, database is CAplus and MEDLINE.

The cytotoxicity of the natural ent-kaurene diterpenoid, oridonin, has been extensively studied. However, the application of oridonin for cancer therapy was hampered primarily by its moderate potency. In this study, a series of oridonin A-ring modified analogs, and their derivatives bearing various substituents on 14-OH position, were designed, synthesized and evaluated for anticancer efficacy. Some of the derivatives were significantly more potent than oridonin against both drug-sensitive and drug-resistant cancer cells. The most potent compound, I, was 200-fold more efficacious than oridonin in MCF-7 cancer cells. Furthermore, I induced apoptosis and cell cycle arrest at the G2/M phase. A decrease in mitochondrial membrane potential and increased Bax/Bcl-2 ratio, accompanied by activated caspase-3 cleavage, were observed in MCF-7 cells after treatment with I, suggesting that the mitochondrial pathway was involved in the I-mediated apoptosis. Moreover, I significantly inhibited tumor growth in mouse xenograft models and had no observable toxic effect.

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 C5H7FO2, Application In Synthesis of 6313-54-8.

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

Isaka, Masahiko published the artcileSemisynthesis and antibacterial activities of nidulin derivatives, Product Details of C6H3ClFNO2, the publication is Journal of Antibiotics (2019), 72(3), 181-184, database is CAplus and MEDLINE.

Derivatives of the fungal depsidone, nidulin, have been synthesized in order to evaluate the potential of the chem. skeleton as antibacterial agents. Alkylation, acylation, and arylation reactions of nornidulin underwent in a regioselective manner to predominantly produce 8-O-substituted derivatives Many of the semisynthetic derivatives showed more potent antibacterial activities than nidulin, In particular, 8-O-aryl ether derivatives displayed significant activities against Gram-pos. bacteria, including Methicillin-resistant Staphylococcus aureus.

Journal of Antibiotics 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

Tian, Jun-Jie published the artcileBorane-Catalyzed Chemoselective and Enantioselective Reduction of 2-Vinyl-Substituted Pyridines, Safety of N-Benzyl-N,N-dibutylbutan-1-aminium chloride, the publication is Angewandte Chemie, International Edition (2020), 59(42), 18452-18456, database is CAplus and MEDLINE.

Herein, we report that highly chemoselective and enantioselective reduction of 2-vinyl-substituted pyridines has been achieved for the first time. The reaction, which uses chiral spiro-bicyclic bisboranes as catalysts and HBpin and an acidic amide as reducing reagents, proceeds through a cascade process involving 1,4-hydroboration followed by transfer hydrogenation of a dihydropyridine intermediate. The retained double bond in the reduction products permits their conversion to natural products and other useful heterocyclic compounds by simple transformations.

Angewandte Chemie, International Edition 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 C19H14O2, Safety of N-Benzyl-N,N-dibutylbutan-1-aminium chloride.

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

Xu, Jun published the artcileMultistep Synthesis and Nematicidal Activity of 2-(8-azabicyclo[3.2.1]octan-3-yl)-3-imino-2,3-dihydro-1H-isoindol-1-One Derivatives, Recommanded Product: 1-(Chloromethyl)-4-(trifluoromethyl)benzene, the publication is Chemistry of Heterocyclic Compounds (New York, NY, United States) (2021), 57(1), 31-39, database is CAplus.

Novel 2-(8-azabicyclo[3.2.1]octan-3-yl)-3-imino-2,3-dihydro-1H-isoindol-1-ones I [R = H, 5-F, 6-MeO, 5-Cl; R¹ = Me, benzyl, 4-chlorobenzyl, etc.; R² = tert-Bu, cyclohexyl, 2-MeOC₆H₄, etc.] which derived from 5-HT₃ receptor antagonists hexahydroazepinylbenzamides were designed and synthesized through isocyanide insertion reaction. All target compounds I were evaluated against pinewood nematodes B. xylophilus and root-knot nematodes M. incognita. Good lethal rate (75%) for I [R = 5-Cl, R¹= Me, R² = tert-butyl] and serious nervous curl effect against pinewood nematodes B. xylophilus for I [R = H, R¹= Me, R² = tert-butyl] were observed at 10 mg/l. The inhibition activities of I [R = H, R¹= Me, R² = 2-MeOC₆H₄, etc.] against root-knot nematodes M. incognita were 84% at 160 mg/l and 60% at 20 mg/l for in-vitro test and test tube test, resp.

Chemistry of Heterocyclic Compounds (New York, NY, United States) published new progress about 939-99-1. 939-99-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzyl chloride,Benzene, name is 1-(Chloromethyl)-4-(trifluoromethyl)benzene, and the molecular formula is C8H17Br, Recommanded Product: 1-(Chloromethyl)-4-(trifluoromethyl)benzene.

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

Xu, Jun published the artcileMultistep Synthesis and Nematicidal Activity of 2-(8-azabicyclo[3.2.1]octan-3-yl)-3-imino-2,3-dihydro-1H-isoindol-1-One Derivatives, Product Details of C7H6Cl2, the publication is Chemistry of Heterocyclic Compounds (New York, NY, United States) (2021), 57(1), 31-39, database is CAplus.

Novel 2-(8-azabicyclo[3.2.1]octan-3-yl)-3-imino-2,3-dihydro-1H-isoindol-1-ones I [R = H, 5-F, 6-MeO, 5-Cl; R¹ = Me, benzyl, 4-chlorobenzyl, etc.; R² = tert-Bu, cyclohexyl, 2-MeOC₆H₄, etc.] which derived from 5-HT₃ receptor antagonists hexahydroazepinylbenzamides were designed and synthesized through isocyanide insertion reaction. All target compounds I were evaluated against pinewood nematodes B. xylophilus and root-knot nematodes M. incognita. Good lethal rate (75%) for I [R = 5-Cl, R¹= Me, R² = tert-butyl] and serious nervous curl effect against pinewood nematodes B. xylophilus for I [R = H, R¹= Me, R² = tert-butyl] were observed at 10 mg/l. The inhibition activities of I [R = H, R¹= Me, R² = 2-MeOC₆H₄, etc.] against root-knot nematodes M. incognita were 84% at 160 mg/l and 60% at 20 mg/l for in-vitro test and test tube test, resp.

Chemistry of Heterocyclic Compounds (New York, NY, United States) 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 C5H10O2S, Product Details of C7H6Cl2.

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

Li, Long-Di published the artcileRoom temperature phosphorescence properties of 27 coumarin derivatives on filter paper, Quality Control of 10543-42-7, the publication is Analytica Chimica Acta (1994), 296(1), 99-105, database is CAplus.

Some coumarin derivatives were used as fluorescence labeling agent. The room temperature phosphorescence (RTP) properties of 27 kinds of coumarin derivatives on filter paper were studied. Most of them can give more intensive RTP signals when using 1.0 mol L^-1 lead acetate as a heavy-atom perturber and there is an obvious relation between the RTP characteristics and the substituting group in some of the derivatives The fact that many of the coumarin derivatives can give RTP emission means that they can be expected to serve as RTP labeling agent.

Analytica Chimica Acta 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, Quality Control of 10543-42-7.

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

Li, Longdi published the artcileRoom temperature phosphorescence properties of 6-coumarinsulfonyl chloride, HPLC of Formula: 10543-42-7, the publication is Fenxi Huaxue (1992), 20(11), 1257-60, database is CAplus.

6-Coumarinsulfonyl chloride (C₆SCl) was used as the fluorescence and low-temperature phosphorescence labeling reagent for amino acids. In this paper, the room-temperature phosphorescence (RPT) of C₆SCl on the several solid substrates, such as filter paper, polyamide films, microcrystalline cellulose, cellulose nitrate, and silica gel for chromatog. etc. was induced successfully by selection of the heavy atom perturbers and exptl. conditions. The RTP emission of C₆SCl has high selectivity, only divalent lead salts are efficient perturber among the examined fifteen compounds and the Pb(OAc)₂ induced the most strong RTP signal. Using 1.0 mol/L Pb(OAc)₂ as the perturber and filter paper as the solid substrate, more intensive RTP signal with high signal to blank ratio was obtained. The RTP signal intensity (λ_x/λ_m = 320/496 nm) as a function of the amount of C₆SCl has a good linear relationship in 0.2 μL sample solution containing 4 to 200 pmol. These results mean that C₆SCl, a new developing luminescence-labeling compound, can be expected to serve as not only a fluorescence labeling reagent, but also a RTP one.

Fenxi Huaxue 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, HPLC of Formula: 10543-42-7.

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

Zhang, Wenwen published the artcileMicrodroplets as Microreactors for Fast Synthesis of Ketoximes and Amides, Related Products of chlorides-buliding-blocks, the publication is Journal of Organic Chemistry (2019), 84(2), 851-859, database is CAplus and MEDLINE.

The formation of amide bonds is one of the most valuable transformations in organic synthesis. Beckmann rearrangement is a well-known method for producing secondary amides from ketoximes. This study demonstrates the rapid synthesis of ketoximes and amides in microdroplets. Many factors are found to affect the yield, such as microdroplet generation devices, temperature, catalysts, and concentrations of reactants. In particular, the temperature has a great influence on the synthesis of amide, which is demonstrated by a sharp ascendance to the yield when the temperature was increased to 45°. The best amide yield (93.3%) can be obtained by using coaxial flowing devices, a sulfonyl chloride compound as a catalyst, and heating to 55° in microdroplets. The yields can reach 78.7-91.3% for benzoylaniline and 87.2-93.4% for benzophenone oximes in several seconds in microdroplets compared to 10.1-66.1% and 82.5-93.3% in several hours in the bulk phase. Apart from the dramatically decreased reaction time and enhanced reaction yields, the microdroplet synthesis is also free of severe reaction environments (anhydrous and anaerobic conditions). In addition, the synthesis in microdroplets also saves reactants and solvents and reduces the waste amounts All of these merits indicate that the microdroplet synthesis is a high-efficiency green methodol.

Journal of Organic Chemistry 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 C11H15NOS, Related Products of chlorides-buliding-blocks.

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

Liu, Ming-Chuan published the artcileSynthesis and cytotoxicity of novel ursolic acid derivatives containing an acyl piperazine moiety, Name: 2-Chloroisonicotinic acid, the publication is European Journal of Medicinal Chemistry (2012), 128-135, database is CAplus and MEDLINE.

This study designed and synthesized a series of novel ursolic acid derivatives in an attempt to develop potent antitumor agents. Their structures were confirmed using MS, IR, ¹H NMR and ¹³C NMR. The inhibitory activities of the title compounds against the MGC-803 (gastric cancer cell) and Bcap-37 (breast cancer cell) human cancer cell lines were evaluated using standard MTT assay in vitro. The pharmacol. results showed that some of the compounds displayed moderate to high levels of antitumor activities against the tested cancer cell lines and that most exhibited more potent inhibitory activities compared with ursolic acid. The mechanism of 2-(4-(2,6-dichlorobenzoyl)piperazin-1-yl)ethyl 3β-hydroxyurs-12-en-28-oate was preliminarily investigated by acridine orange/ethidium bromide staining, Hoechst 33258 staining, TUNEL assay and flow cytometry, which revealed that the compound can induce cell apoptosis in MGC-803 cells.

European 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, Name: 2-Chloroisonicotinic acid.

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

Dong, Yanan published the artcileReductive cyanation of organic chlorides using CO₂ and NH₃ via Triphos-Ni(I) species, COA of Formula: C12H15ClO3, the publication is Nature Communications (2020), 11(1), 4096, database is CAplus and MEDLINE.

The reductive cyanation of organic chlorides RCl (R = C₆H₅, naphthalen-1-yl, cyclohexyl, etc.) using CO₂/NH₃ as the electrophilic CN source has been described. The use of tridentate phosphine ligand Triphos allows for the nickel-catalyzed cyanation of a broad array of aryl and aliphatic chlorides to produce the desired nitrile products RCN in good yields, and with excellent functional group tolerance. Cheap and bench-stable urea was also shown as suitable CN source, suggesting promising application potential. Mechanistic studies imply that Triphos-Ni(I) species are responsible for the reductive C-C coupling approach involving isocyanate intermediates. This method expands the application potential of reductive cyanation in the synthesis of functionalized nitrile compounds under cyanide-free conditions, which is valuable for safe synthesis of (isotope-labeled) drugs.

Nature Communications published new progress about 637-07-0. 637-07-0 belongs to chlorides-buliding-blocks, auxiliary class Inhibitor,Cell Cycle,PPAR, name is Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate, and the molecular formula is C12H15ClO3, COA of Formula: C12H15ClO3.

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