Month: November 2022

Shen, Gang published the artcilePhospholipid Conjugate for Intracellular Delivery of Peptide Nucleic Acids, HPLC of Formula: 186046-83-3, the publication is Bioconjugate Chemistry (2009), 20(9), 1729-1736, database is CAplus and MEDLINE.

Peptide nucleic acids (PNAs) have a number of attractive features that have made them an ideal choice for antisense and antigene-based tools, probes, and drugs, but their poor membrane permeability has limited their application as therapeutic or diagnostic agents. Herein, we report a general method for the synthesis of phospholipid-PNAs (LP-PNAs) and compare the effect of noncleavable lipids and bioreductively cleavable lipids (L and LSS) and phospholipid (LP) on the splice-correcting bioactivity of a PNA bearing the cell penetrating Arg9 group (PNA-R9). While the three constructs show similar and increasing bioactivity at 1-3 μM, the activity of LP-PNA-R9 continues to increase from 4-6 μM, while the activity of L-PNA-R9 remains constant and that of LSS-PNA-R9 decreases rapidly in parallel with their relative cytotoxicity. The activity of both LP-PNA-R9 and L-PNA-R9 dramatically increased in the presence of chloroquine, as expected for an endocytic entry mechanism. The constructs were also found to have CMC values of 1.0 and 4.5 μM, resp., in 150 mM NaCl, pH 7 water, suggesting that micelle formation may play a hitherto unrecognized role in modulating toxicity and/or facilitating endocytosis.

Bioconjugate Chemistry published new progress about 186046-83-3. 186046-83-3 belongs to amides-buliding-blocks, auxiliary class Purine,Carboxylic acid,Amine,Benzene,Amide,Others,PNA,, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, and the molecular formula is C19H14N2, HPLC of Formula: 186046-83-3.

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

Li, Yue published the artcileAn in-line capillary electrophoresis assay for the high-throughput screening of histone deacetylase inhibitors, Safety of H-Lys(Boc)-OH, the publication is Journal of Chromatography A (2019), 171-177, database is CAplus and MEDLINE.

Histone deacetylases (HDACs) are important enzymes that cause chromatin structure contraction and transcription repression, which can downregulate some cancer-suppression genes and lead to the occurrence of cancer. HDAC-specific inhibition is an effective approach to cancer therapy. Hence, a method with which to investigate HDAC activity is needed. We developed an in-line capillary electrophoresis method based on electrophoretically mediated microanal. The optimized conditions were thoroughly validated, and the method was applied to determine the enzyme’s kinetic parameters and the inhibition characteristics of three potent probe inhibitors. The obtained values were comparable to the literature data. Hence, the presented method, with its advantages of miniaturization and full automation, could be used for kinetic and inhibition studies of HDACs, which are targets for drug discovery, in the early stages of new drug development.

Journal of Chromatography A published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Safety of H-Lys(Boc)-OH.

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

Bryson, David I. published the artcileContinuous directed evolution of aminoacyl-tRNA synthetases, Name: H-Lys(Boc)-OH, the publication is Nature Chemical Biology (2017), 13(12), 1253-1260, database is CAplus and MEDLINE.

Directed evolution of orthogonal aminoacyl-tRNA synthetases (AARSs) enables site-specific installation of noncanonical amino acids (ncAAs) into proteins. Traditional evolution techniques typically produce AARSs with greatly reduced activity and selectivity compared to their wild-type counterparts. We designed phage-assisted continuous evolution (PACE) selections to rapidly produce highly active and selective orthogonal AARSs through hundreds of generations of evolution. PACE of a chimeric Methanosarcina spp. pyrrolysyl-tRNA synthetase (PylRS) improved its enzymic efficiency (k_cat/K_M^tRNA) 45-fold compared to the parent enzyme. Transplantation of the evolved mutations into other PylRS-derived synthetases improved yields of proteins containing noncanonical residues up to 9.7-fold. Simultaneous pos. and neg. selection PACE over 48 h greatly improved the selectivity of a promiscuous Methanocaldococcus jannaschii tyrosyl-tRNA synthetase variant for site-specific incorporation of p-iodo-L-phenylalanine. These findings offer new AARSs that increase the utility of orthogonal translation systems and establish the capability of PACE to efficiently evolve orthogonal AARSs with high activity and amino acid specificity.

Nature Chemical Biology published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Name: H-Lys(Boc)-OH.

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

Rich, Rebecca L. published the artcileBiacore analysis with stabilized G-protein-coupled receptors, Recommanded Product: N-(4-Acetylphenyl)-2-(4-(2,6-dioxo-1,3-dipropyl-2,3,6,9-tetrahydro-1H-purin-8-yl)phenoxy)acetamide, the publication is Analytical Biochemistry (2011), 409(2), 267-272, database is CAplus and MEDLINE.

Using stabilized forms of β₁ adrenergic and A_2A adenosine G-protein-coupled receptors, we applied Biacore to monitor receptor activity and characterize binding constants of small-mol. antagonists spanning more than 20,000-fold in affinity. We also illustrate an improved method for tethering His-tagged receptors on NTA (carboxymethylated dextran preimmobilized with nitrilotriacetic acid) chips to yield stable, high-capacity, high-activity surfaces as well as a novel approach to regenerate receptor binding sites. Based on our success with this approach, we expect that the combination of stabilized receptors with biosensor technol. will become a common method for characterizing members of this receptor family.

Analytical Biochemistry published new progress about 264622-53-9. 264622-53-9 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Adenosine Receptor, name is N-(4-Acetylphenyl)-2-(4-(2,6-dioxo-1,3-dipropyl-2,3,6,9-tetrahydro-1H-purin-8-yl)phenoxy)acetamide, and the molecular formula is C27H29N5O5, Recommanded Product: N-(4-Acetylphenyl)-2-(4-(2,6-dioxo-1,3-dipropyl-2,3,6,9-tetrahydro-1H-purin-8-yl)phenoxy)acetamide.

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

Eroglu, Zuhal published the artcileEffect of SIRT1 activators and inhibitors on CD44⁺/CD133⁺-enriched non.small cell lung cancer cells, Safety of 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide, the publication is Molecular Medicine Reports (2020), 22(1), 575-581, database is CAplus and MEDLINE.

Lung cancer is one of the most commonly diagnosed cancers and it is associated with high rates of morbidity and mortality. Metastasis and relapse of the tumor depend on the survival and proliferation of lung cancer stem cells (LC SCs). The ability to identify CSCs may prevent recurrence and lead to more effective treatments. Sirtuins are a group of deacetylases that include seven variants (SIRT1-7), with sirtuin 1 (SIRT1) being the most intensively investigated. Evidence suggests that SIRT1 is both a tumor-suppressor gene and an oncogene. SIRT1 can deacetylate the tumor-suppressor protein p53 to decrease its activity. SIRT1 activators increase the deacetylation of p53, whereas SIRT1 inhibitors can stimulate p53 by inhibiting deacetylation. In the present study, CD 44⁺ and CD 133⁺-enriched A549 (non-small cell lung cancer) cells collected using the CD 44 and CD 133 CSC surface markers by fluorescence-activated cell sorting method were treated with SIRT1 inhibitors (tenovin-6 and sirtinol) and SIRT1 activators (resveratrol and SRT1720), and their effects on apoptosis, as well as the mRNA and protein expression of SIRT1 and p53 were investigated. Of these agents, it was found that resveratrol increased p53 expression by 4.1-fold, decreased SIRT1 expression by 0.2-fold, and it was the most potent inducer of apoptosis.

Molecular Medicine Reports published new progress about 1011557-82-6. 1011557-82-6 belongs to amides-buliding-blocks, auxiliary class Epigenetics,Sirtuin, name is 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide, and the molecular formula is C25H34N4O2S, Safety of 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide.

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

Wong, Anthony published the artcileTissue-Reparative Benefits of MST1/2 Inhibition: Separating the Wheat From the Chaff, Product Details of C12H23N3S, the publication is Circulation Research (2021), 129(10), 927-929, database is CAplus and MEDLINE.

Identifying potential therapeutic targets for tissue repair following injury such as myocardial infarction (Ml) is a difficult task given the need to maintain the temporal balance of acute inflammation and resolution post-MI. Using XMU-MP-1 to inhibit MST1/2 activity, they found increased tissue fibrosis, left ventricular dilation, tissue fibrosis, inflammatory cytokine production, mortality, and decreased cardiac function. Importantly, pharmacol. inhibition of LTB4 alone had no effect, but when combined with XMU-MP-1 treatment, blockade of both MST1/2 and LTB4 ameliorated cardiac function and adverse tissue remodeling post-MI.

Circulation Research published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C13H14BNO2, Product Details of C12H23N3S.

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

Isley, Nicholas A. published the artcileTotal Synthesis and Stereochemical Assignment of Streptide, Recommanded Product: H-Lys(Boc)-OH, the publication is Journal of the American Chemical Society (2019), 141(43), 17361-17369, database is CAplus and MEDLINE.

Streptide is a peptide-derived macrocyclic natural product that has attracted considerable attention since its discovery in 2015. It contains an unprecedented post-translational modification that intramolecularly links the β-carbon (C3) of a residue 2 lysine with the C7 of a residue 6 tryptophan, thereby forming a 20-membered cyclic peptide. Herein, we report the first total synthesis of streptide that confirms the regiochem. of the lysine-tryptophan crosslink and provides an unambiguous assignment of the stereochem. (3R vs 3S) of the lysine-2 C3 center. Both the 3R and the originally assigned 3S lysine diastereomers were independently prepared by total synthesis and it is the former, not the latter, that was found to correlate with the natural product. The approach enlists a powerful Pd(0)-mediated indole annulation for the key macrocyclization of the complex core peptide, utilizes an underdeveloped class of hypervalent iodine(III) aryl substrates in a palladium-catalyzed C-H activation/β-arylation reaction conducted on a lysine derivative, and provides access to material with which the role of streptide and related natural products may be examined

Journal of the American Chemical Society published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Recommanded Product: H-Lys(Boc)-OH.

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

Yahya, Rana published the artcileRecycling Oryza sativa wastes into poly-imidazolium acetic acid-tagged nanocellulose Schiff base supported Pd nanoparticles for applications in cross-coupling reactions, Name: 2-Chloroacetamide, the publication is Reactive & Functional Polymers (2022), 105137, database is CAplus.

A green and sustainable heterogeneous nanocatalyst for the Suzuki reaction was fabricated by refining rice straw to ionic nanocellulose Schiff base (NCESB) which was employed for bio-reduction of Pd(II) into Pd nanoparticles (Pd NPs) and immobilization of these NPs to fabricate the desired nanocatalyst (NCESB@Pd). The TEM image revealed well-dispersed PdNPs with sizes of 5-23 nm. The new nanocatalyst displayed amazing activity in catalyzing coupling reactions of a wide range of halobenzenes with phenylboronic acid at 50°C (reaction time 15-60 min) and even at room temperature (reaction time 120 min). The NCESB@Pd nanocatalyst exhibited excellent recyclability (up to five catalytic runs) without a significant loss of its activity or identity. Therefore, the new ionic nanocatalyst may open a new window for a novel generation of ionic low-cost green and highly effective nanocatalysts for organic transformation reactions.

Reactive & Functional Polymers published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C10H15NS, Name: 2-Chloroacetamide.

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

Hassan, Aisha Y. published the artcilePotential antiviral and anticancer effect of imidazoles and bridgehead imidazoles generated by HPV-Induced cervical carcinomas via reactivating the P53/pRb pathway and inhibition of CA IX, Application of 2-Chloroacetamide, the publication is Journal of Molecular Structure (2021), 129865, database is CAplus.

Human papillomaviruses E6 and E7 oncoproteins are crucial to viral-induced cervical cancers and targeting E6/E7 leads to safer and better treatment for cervical cancer. Hence, a simple and green solvent-free protocol was applied for the synthesis of novel imidazoles e.g., I, and bridgehead imidazoles (purine analogs), e.g., II, via versatile straightforward synthetic routes. All the synthesized compounds have been characterized by IR, ¹H NMR, ¹³C NMR, mass spectroscopy, and elemental analyses and then have been examined for their in vitro antiviral activity against HPV, genotype 18. Two compounds, I and II, were the most promising HR-HPV inhibitors with a percentage of 95.00 and 96.84%, resp. Both compounds demonstrated a substantial down-regulation of HPV oncoproteins E6 and E7 with up-regulation of tumor suppressor proteins, p53, and pRb, resp. using western blot technique. Furthermore, the cytotoxicity of compounds I and II against the cervical cancer Hela cell line was further examined Compound I exhibited strong anticancer activity with IC₅₀ 0.08μM, which is equivalent to 5-FU (IC₅₀ 0.09μM). The cell cycle anal. was performed for investigating the potential mechanism of compound I, resulting in a significant accumulation of the cell population in both pre-G1 and G0-G1 phases and arrest the cell cycle at G1 phase. Addnl., compound I induced apoptosis, triggering cell death via increasing the early and late apoptotic rates by approx. 16 and 188 folds compared with the control. The most cytotoxic agent, I, revealed a remarkable inhibition of the targeted carbonic anhydrase IX enzyme with an IC₅₀ value of 0.12μM comparable to the standard drug. In addition, the ADME profiles of the most highly successful derivatives have been studied in order to determine their ability to be produced as good drug candidates.

Journal of Molecular Structure published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Application of 2-Chloroacetamide.

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

El-Faham, Ayman published the artcileSynthesis, characterization and anti-proliferation activity of novel cyano oximino sulfonate esters, Name: 2-Cyano-N-ethylacetamide, the publication is Chemical & Pharmaceutical Bulletin (2014), 62(4), 373-378, database is CAplus and MEDLINE.

A series of cyano oximino sulfonate derivatives RS(O)2ON:C(CN)X (R = 4-CH₃C₆H₅, naphthalen-2-yl; X = C₆H₅, C₂H₅NH₂, NH₂, etc). were prepared from the reaction of arylsulfonyl chloride with different cyanoacetamide-based oximes ranging from the simplest unsubstituted amide to analogs containing N-Et (mimicking the Oxyma template), N-piperidinyl and N-morpholinyl chains. In addition, the cyano oximes, N-hydroxybenzimidoyl cyanide and N-hydroxy picolinimidoyl cyanide were also used in the synthesis of cyano oximino sulfonate derivatives The preliminary bioassays showed that some of the title compounds, such as (TsPipOx), (TsPhOX), (NpsPipOx) etc, showed anti-proliferation effect on the mouse fibroblast L929. The calculated IC₅₀-values were ranging between 36.5 μg/mL and 0.235 mg/mL. However the anti-proliferation effects seem to be cytostatic rather than cytotoxic. The compounds only minimize the growth activity without completely killing the cells.

Chemical & Pharmaceutical Bulletin published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C5H8N2O, Name: 2-Cyano-N-ethylacetamide.

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