Month: December 2022

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

A highly efficient Rh(III)-catalyzed cascade C-H activation/annulation of sulfoximines 2-R-3-R1-4-R2C6H2S(O)(=NH)R3 (R = H, Me, OMe, Cl, Br; R1 = H, Me, OMe, Br, NO2; R2 = H, F, CN, C(O)Me, etc.; R1R2 = -CH=CH-CH=CH-; R3 = Me, Et, Bn, etc.) with iodonium ylides I (n = 0, 1; R4 = H, Me, Ph; R5 = H, Me) under metal-oxidant-free conditions has been reported. The fused cyclohexanone-1,2-benzothiazine scaffolds II is readily achieved with a one-pot process in this reaction. This protocol exhibits good functional group tolerance and moderate to excellent yields. Addnl., the olefination of the target product II (n = 1; R = R1 = R2 = H; R3 = Me; R4 = R5 = H) illustrates the promising usefulness of this strategy.

Rhodium(III)-catalyzed cascade C-H functionalization/annulation of sulfoximines with iodonium ylides for the synthesis of cyclohexanone-1,2-benzothiazines. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

A practical method for the synthesis of ¦Á-ketoamides of sulfoximines I [R1 = Ph, 4-MeC6H4, Bn, etc.; R2 = Me, Et, Ph, etc.; R3 = H, 4-F, 2-Cl, etc.] was developed from NH-sulfoximines and acetophenones using selenium dioxide as an oxidant. The reactions proceeded under mild conditions in the absence of any additives and provided good to excellent yields of ¦Á-keto-N-acylsulfoximines. Moreover, the optimized condition was well-suited to the task of ¦Á-ketoacylation of sulfoximines with phenylacetaldehyde and arylacetylenes. ¦Á-Hydroxy N-acylsulfoximines were obtained in good yields from ¦Á-keto N-acylsulfoximines via reduction or Grignard reactions.

Selenium Dioxide Promoted ¦Á-Keto N-Acylation of Sulfoximines Under Mild Reaction Conditions. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Iminotetrahydrothiophene 1-oxide (BD00963737) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

An efficient and metal-free method for the construction of ¦Á-diarylmethine imino sulfanones e.g., I using acid-catalyzed 1,6-conjugate addition of sulfoximines e.g., II on para-quinine methides III (R = Ph, 4-fuloropheny, thiophen-2-yl, etc. R1 = Me, t-Bu) (p-QMs) was reported. This method showed broad functional group tolerance and a wide range of substrate scope with good to excellent yield. The excellent protocol exhibits mild reaction conditions with high atom economy. The practicability of the present method was supported by a Gram-scale reaction.

Metal-Free, Acid-Catalyzed 1,6-Conjugate Addition of NH-Sulfoximines to para-Quinone Methides: Accessing to Diarylmethine Imino Sulfanone. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. Trivial name: delta-Cadinene.
2. It’s mainly derived from flue-cured tobacco, burley tobacco and flavoured tobacco, it has a strong aroma and a good fixing effect, suitable for perfume, cosmetics, can also be used in wine, cigarettes, and toothpaste.
. Recommended Products is: 29350-73-0 and 51905-84-1.

This study analyzed the chem. composition and anti-osteoporosis activity of the n-hexane extract of Homalomena gigantea rhizome. Sixty compounds, representing 92.0% of the extract, were identified by gas chromatog.-mass spectrometry. Linalool (15.3%), oplopanone (9.8%), (¦¥)-¦Á-atlantone (5.6%), khusinol acetate (5.4%), bullatantriol (4.3%), and ¦Â-sitosterol (3.8%) were the main constituents. The anti-osteoporotic activity of the n-hexane extract was determined by measuring alk. phosphatase (ALP) activity, collagen content, and the mineralization of MC3T3-E1 cells. At concentrations of 4.0 and 20.0 ¦Ìg/mL, the n-hexane extract increased ALP activity by 8.2% and 23.7%, and increased collagen secretion by MC3T3-E1 cells by 114.9% and 112.4%, resp. At 4 ¦Ìg/mL, the extract significantly promoted the mineralization of MC3T3-E1 cells by as much as 133.2% compared to the neg. control. These results suggested that H. gigantea rhizome contains a natural anti-osteoporotic compound

Volatile Constituents and Anti-Osteoporotic Activity of the n-Hexane Extract From Homalomena gigantea Rhizome. Recommended basis is Cadinene. Products is: https://www.ambeed.com/products/189165-77-3.html, 51905-84-1

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(2S)-2-Amino-4-(butylsulfonimidoyl)butanoic acid (BD136012) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 1621962-30-8.

8-Epidiosbulbin E acetate (EEA), a furan-containing diterpenoid lactone, is one of main component of Dioscorea bulbifera L.(DBL). It has been reported that EEA induces severe hepatotoxicity in mice and that its hepatotoxicity is associated with metabolic activation. The present study demonstrated that exposure to EEA (50, 100 or 200 ¦ÌM) induced DNA damage, including significant DNA fragmentation, increases of tail DNA and olive tail moment, H2AX phosphorylation and PARP-1 activation, in cultured mouse primary hepatocytes. Similar observation was obtained in mice administered EEA at 50, 100 or 200 mg/kg. Pre-treatment with 10 ¦ÌM ketoconazole (KTC), 200 ¦ÌM vitamin C (VC), or 200 ¦ÌM glutathione Et ester (GSH-OEt) reversed the over-production of reactive oxygen species (ROS) induced by EEA and attenuated susceptibility of hepatocytes to EEA-induced cytotoxicity and DNA damage in mouse primary hepatocytes. In contrast, pre-treatment with 1.0 mM L-buthionine sulfoximine (BSO) potentiated over-production of ROS, cytotoxicity and DNA damage induced by EEA. In summary, EEA induced DNA damage in cultured primary hepatocytes and the liver of mice. ROS, possibly along with DNA alkylation, participated in the observed DNA damage.

DNA damage by reactive oxygen species resulting from metabolic activation of 8-epidiosbulbin E acetate in vitro and in vivo. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(S-Methylsulfonimidoyl)benzene (BD302898) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 83730-53-4 and 1621962-30-8.

A Ru(II)-catalyzed enantioselective C-H activation/annulation of sulfoximines with ¦Á-carbonyl sulfoxonium ylides using a novel class of chiral binaphthyl monocarboxylic acids as chiral ligands, which can be easily and modularly prepared from 1,1′-binaphthyl-2,2′-dicarboxylic acid to give benzo[e][1,2]thiazine 1-oxide derivatives I [R = i-Pr, 2-furyl, Ph, etc.; Ar = Ph, 3-ClC6H4, 4-F3CC6H4, 2-FC6H4, etc.] was described. A broad range of sulfur-stereogenic sulfoximines were prepared in high yields with excellent enantioselectivities (up to 99% yield and 99% ee) via desymmetrization, kinetic resolution, and parallel kinetic resolution Furthermore, the resolution products can be easily transformed to chiral sulfoxides and key intermediates for kinase inhibitors.

Efficient Synthesis of Sulfur-Stereogenic Sulfoximines via Ru(II)-Catalyzed Enantioselective C-H Functionalization Enabled by Chiral Carboxylic Acid. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. Trivial name: delta-Cadinene.
2. It’s mainly derived from flue-cured tobacco, burley tobacco and flavoured tobacco, it has a strong aroma and a good fixing effect, suitable for perfume, cosmetics, can also be used in wine, cigarettes, and toothpaste.
. Recommended Products is: 29350-73-0 and 51905-84-1.

In this study, we produced roasted, baked, steamed, and sun-dried green tea products using the same batch of fresh tea leaves (FTL) of Longjing 43 (Camellia sinensis var. sinensis), and explored processing effects on the metabolic profiles of four types of green teas (FGTs) using the widely targeted metabolomics. Results showed that 146 differential metabolites including flavonoids, amino acids, lipids, and phenolic acids were screened among 1034 non-volatiles. In addition, nineteen differential metabolites were screened among 79 volatiles. Most of non-volatiles and volatiles metabolites changed notably in different manufacturing processes, whereas there were no significant differences (p>0.05) in the levels of total catechins between FGTs and FTL. The transformation of metabolites was the dominant trend during green tea processing. The results contribute to a better understanding of how the manufacturing process influences green tea quality, and provide useful information for the enrichment of tea biochem. theory.

Comprehensive investigation on non-volatile and volatile metabolites in four types of green teas obtained from the same tea cultivar of Longjing 43 (Camellia sinensis var. sinensis) using the widely targeted metabolomics. Recommended basis is Cadinene. Products is: https://www.ambeed.com/products/189165-77-3.html, 51905-84-1

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(2S)-2-Amino-4-(butylsulfonimidoyl)butanoic acid (BD136012) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 1621962-30-8.

Arsenic is an environmental chem. of toxicol. concern today since it is a human genotoxin and chronic exposure is associated with development of cancers, including skin. Inorganic arsenate is metabolically reduced to arsenite by glutathione (GSH) prior to methylation. The aim of this study was to determine the relative toxic effects of arsenate and arsenite in HaCat cells (immortalized human keratinocytes) in vitro by measuring cytotoxicity, DNA damage, depletion of glutathione and apoptotic and necrotic events. HaCat cells were treated with arsenate and arsenite (10¦ÌM) for DNA damage detection using Comet assay and cytotoxicity (10, 60 and 100¦ÌM) all measured at 24 h. In some experiment arsenate or arsenite (10¦ÌM) was added at the same time as BSO 10¦ÌM for 24 h, and GSH levels were measured by HPLC with fluorescence detection. Flow cytometry was used to investigate apoptotic and necrotic events following arsenate and arsenite (10¦ÌM) treatment for 24 h. Arsenate and arsenite at 60 and 100¦ÌM, but not 10¦ÌM, reduced the number of adherent viable cells with time. Therefore, DNA damage could only be measured at 10¦ÌM as at higher concentrations the cells did not produce classical Comets but showed fragmentation. DNA damage was significantly (p < 0.001) increased in cells treated for 24 h with 10¦ÌM arsenate and arsenite compared to control. GSH levels were significantly increased in HaCat cells treated with10¦ÌM arsenate and arsenite (p <0.05, p < 0.001, resp.) compared to control. Cells treated with buthionine sulfoximine (BSO) at the same time as arsenate had increased GSH levels (p < 0.001), but arsenite and BSO did not increase cellular GSH. Arsenate and arsenite increased apoptosis, and arsenate increased necrosis, although none of the values reached statistical significance. Arsenite was more cytotoxic than arsenate. Arsenate and arsenite are known to produce oxidative stress involving ROS formation and depletion of glutathione. The increase in GSH levels at low doses of arsenate and arsenite, and by arsenate even in the presence of BSO. Genotoxic effect of arsenate and arsenite in human hacat cells in culture using comet assay. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(S-Methylsulfonimidoyl)benzene (BD302898) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 83730-53-4 and 1621962-30-8.

This work reports a novel and efficient palladium-catalyzed synthesis of tricyclic dibenzothiazines using easily prepared aryl sulfoximines and aryne precursors via C-H functionalization and cyclization. A mechanistic investigation indicated that the C-H bond cleavage at the position ortho to the sulfoximine group is the rate-determining step.

Palladium-Catalyzed Oxidative Annulation of Sulfoximines and Arynes by C-H Functionalization as an Approach to Dibenzothiazines. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(S-Methylsulfonimidoyl)benzene (BD302898) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 83730-53-4 and 1621962-30-8.

Upon application of a multicomponent Petasis reaction, a broad range of NH-sulfoximines R1R2S(O)=NH (R1 = Ph, naphthalen-2-yl; R2 = Me, Ph, cyclopentyl, etc.) and boronic acids R3C6H5B(OH)2 (R3 = H, 4-Me, 3-SMe, 4-F, etc.) react with glyoxalic acid to afford the corresponding 2-substituted acetic acids with N-bound sulfoximidoyl groups R1R2S(O)=NCH2(R3)C(O)O(R4) (R4 = H, Me). The protocol features excellent yields under ambient, metal-free conditions and short reaction times. Furthermore, the applicability of 2-sulfoximidoyl acetic acids as building blocks for synthesizing sulfoximine-based benzodiazepine analogs (1R,3R)/(1S,3R)-I was demonstrated.

2-Sulfoximidoyl Acetic Acids from Multicomponent Petasis Reactions and Their Use as Building Blocks in Syntheses of Sulfoximine Benzodiazepine Analogues. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem