Month: December 2022

Eto, Shotaro published the artcileAnti-tumor effects of the histone deacetylase inhibitor vorinostat on canine urothelial carcinoma cells, HPLC of Formula: 1011557-82-6, the publication is PLoS One (2019), 14(6), e0218382, database is CAplus and MEDLINE.

Canine urothelial carcinoma (cUC) is the most common tumor of the lower urinary tract in dogs. Although chemotherapy and radical surgery have improved the overall survival, most dogs with cUC succumb to metastasis or recurrence. Therefore, the development of an effective systematic therapy is warranted. In this study, a comprehensive drug screening test using a cUC cell line was performed and the anti-tumor effect of a histone deacetylase (HDAC) inhibitor was evaluated. Comprehensive drug screening was performed on cUC cells. Based on this screening, the anti-proliferation effect of vorinostat, an HDAC inhibitor clin. applied in humans, was evaluated using several cUC cell lines in sulforhodamine B and flow cytometry assays. Western blot anal. was also performed to evaluate the degree of acetylation of histone H3 as well as the expression and phosphorylation of cell cycle-related mols. The anti-tumor effect of vorinostat in vivo was evaluated using a xenograft model. Finally, immunohistochem. was performed on acetyl-histone H3 in cUC and the relationship between the degree of acetylation and prognosis was examined using Kaplan-Meier survival anal. Drug screening revealed that HDAC inhibitors consistently inhibited the growth of cUC cells. Vorinostat inhibited the growth of 6 cUC cell lines in a dose-dependent manner and induced G0/G1 cell cycle arrest. Western blot anal. showed that vorinostat mediated the acetylation of histone H3, the dephosphorylation of p-Rb, and the upregulation of p21 upon exposure to vorinostat. Furthermore, inhibition of tumor growth was observed in the xenograft model. In clin. cUC cases, neoplastic urothelium showed significant deacetylation of histones compared to the normal control, where lower histone acetylation levels were associated with a poor prognosis. In conclusion, the therapeutic potential of vorinostat was demonstrated in cUC. Histone deacetylation may be related to cUC tumor progression.

PLoS One 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, HPLC of Formula: 1011557-82-6.

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

Brownlee, R. T. C. published the artcileNatural abundance nitrogen-15 chemical shifts in substituted benzamides and thiobenzamides, Formula: C8H9NOS, the publication is Magnetic Resonance in Chemistry (1986), 24(9), 821-6, database is CAplus.

¹⁵N substituent chem. shifts (measured at natural abundance at 0.4 M concentration) and calculated (ab initio, STO-3G) electron densities at the N and O (or S) are reported for series of para- and meta-substituted benzamides and thiobenzamides with NMe₂, NH₂, OMe, NHCOMe, F, Cl, Br, I, Me, H, COMe, CO₂Me, CF₃, CN, NO₂, CONH₂ and CSNH₂ substituents. The ¹⁵N shifts are very sensitive to the substituent effects. The dual substituent parameter method shows excellent correlations of ¹⁵N shifts against substituent field and resonance effects, with the sensitivity in the thiobenzamides being double that in the benzamides. In contrast, calculated π-electron densities at the N show the same sensitivity to substituents in both series. The ¹⁵N shifts correlate well with the calculated π-electron densities at the N; however, estimates of the shielding based on local electron densities (described in Pople’s independent electron model) cannot account for the increased sensitivity to the substituent effects observed for ¹⁵N chem. shifts of thiobenzamides. It is suggested that nonlocal shielding from S and O are responsible for the chem. shift trends.

Magnetic Resonance in Chemistry published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C8H9NOS, Formula: C8H9NOS.

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

Yashaswini, Puttaraju Srikantamurthy published the artcileIn vivo modulation of LPS induced leukotrienes generation and oxidative stress by sesame lignans, Name: [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Journal of Nutritional Biochemistry (2017), 151-157, database is CAplus and MEDLINE.

The role of inflammation and oxidative stress is critical during onset of metabolic disorders and this has been sufficiently established in literature. In the present study, we evaluated the effects of sesamol and sesamin, two important bioactive mols. present in sesame oil, on the generation of inflammatory and oxidative stress factors in LPS injected rats. Sesamol and sesamin lowered LPS induced expression of cPLA₂ (61 and 56%), 5-LOX (44 and 51%), BLT-1(32 and 35%) and LTC₄ synthase (49 and 50%), resp., in liver homogenate. The diminished serum LTB₄ (53 and 64%) and LTC₄ (67 and 44%) levels in sesamol and sesamin administered groups, resp., were found to be concurrent with the observed decrease in the expression of cPLA₂ and 5-LOX. The serum levels of TNF-α (29 and 19%), MCP-1 (44 and 57%) and IL-1β (43 and 42%) were found to be reduced in sesamol and sesamin group, resp., as given in parentheses, compared to LPS group. Sesamol and sesamin offered protection against LPS induced lipid peroxidation in both serum and liver. Sesamol, but not sesamin, significantly restored the loss of catalase and glutathione reductase activity due to LPS (P<.05). However, both sesamol and sesamin reverted SOD activities by 92 and 98%, resp. Thus, oral supplementation of sesamol and sesamin beneficially modulated the inflammatory and oxidative stress markers, as observed in the present study, in LPS injected rats. Our report further advocates the potential use of sesamol and sesamin as an adjunct therapy wherein, inflammatory and oxidative stress is of major concern.

Journal of Nutritional Biochemistry 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 C14H28O5S, Name: [(2-Hexylcyclopentylidene)amino]thiourea.

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

Ozuna, Lorena Miss published the artcileDupilumab-associated arthralgia in patients with aspirin-exacerbated respiratory disease, Synthetic Route of 169590-42-5, the publication is Annals of Allergy, Asthma, & Immunology (2022), 128(4), 469-472, database is CAplus and MEDLINE.

Dupilumab is generally safe and well-tolerated; however, in a phase 3 clin. trial of dupilumab for CRSwNP, arthralgias were reported 4.7% and 7.4% of patients in the treatment arms compared with 1.3% of patients in the placebo arm. In this study, we evaluate the clin. characteristics and outcomes of 8 patients with AERD who developed arthralgias after initiating dupilumab. Of 160 patients with AERD treated with dupilumab at our center, we identified 8 patients (5.0%) who reported possible dupilumab-associated arthralgias at their allergy and immunol. follow-up visit. Several patients sought treatment for the arthralgias and were prescribed celecoxib or oral and intra-articular corticosteroids. Of the 8 patients, 5 had spontaneous resolution of their pain after an average of 6.9 mo, whereas arthralgias in 3 patients remain unresolved. Furthermore, our clin. outcomes were limited to the evaluations performed by the clinician caring for the patient and not all patients had a complete inflammatory and rheumatol. workup for their symptoms. Joint symptoms are very common in adults and may have been unrelated to dupilumab. Lastly, the mechanism of dupilumab-associated arthralgias is not clear, but a possible mechanism is a shift toward a type 1 or type 3 immune profile which may be indicative of a type 1 or type 3 “escape” with inhibition of IL-4Ra. Further studies to under-stand the mechanism of dupilumab-associated arthralgias are warranted. Clinicians caring for patients with AERD encountering this adverse effect should use shared decision-making to determine whether patients can continue dupilumab with close follow-up.

Annals of Allergy, Asthma, & Immunology published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, Synthetic Route of 169590-42-5.

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

Patil, Prarthana published the artcileReactive oxygen species-degradable polythioketal urethane foam dressings to promote porcine skin wound repair, Safety of 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide, the publication is Science Translational Medicine (2022), 14(641), eabm6586, database is CAplus and MEDLINE.

Porous, resorbable biomaterials can serve as temporary scaffolds that support cell infiltration, tissue formation, and remodeling of nonhealing skin wounds. Synthetic biomaterials are less expensive to manufacture than biol. dressings and can achieve a broader range of physiochem. properties, but opportunities remain to tailor these materials for ideal host immune and regenerative responses. Polyesters are a well-established class of synthetic biomaterials; however, acidic degradation products released by their hydrolysis can cause poorly controlled autocatalytic degradation Here, we systemically explored reactive oxygen species (ROS)-degradable polythioketal (PTK) urethane (UR) foams with varied hydrophilicity for skin wound healing. The most hydrophilic PTK-UR variant, with seven ethylene glycol (EG7) repeats flanking each side of a thioketal bond, exhibited the highest ROS reactivity and promoted optimal tissue infiltration, extracellular matrix (ECM) deposition, and reepithelialization in porcine skin wounds. EG7 induced lower foreign body response, greater recruitment of regenerative immune cell populations, and resolution of type 1 inflammation compared to more hydrophobic PTK-UR scaffolds. Porcine wounds treated with EG7 PTK-UR foams had greater ECM production, vascularization, and resolution of proinflammatory immune cells compared to polyester UR foam-based NovoSorb Biodegradable Temporizing Matrix (BTM)-treated wounds and greater early vascular perfusion and similar wound resurfacing relative to clin. gold standard Integra Bilayer Wound Matrix (BWM). In a porcine ischemic flap excisional wound model, EG7 PTK-UR treatment led to higher wound healing scores driven by lower inflammation and higher reepithelialization compared to NovoSorb BTM. PTK-UR foams warrant further investigation as synthetic biomaterials for wound healing applications.

Science Translational Medicine published new progress about 1869-45-0. 1869-45-0 belongs to amides-buliding-blocks, auxiliary class Trifluoromethylated Building Blocks, name is 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide, and the molecular formula is C4H6F3NOS, Safety of 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide.

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

Medda, Federico published the artcileNovel Cambinol Analogs as Sirtuin Inhibitors: Synthesis, Biological Evaluation, and Rationalization of Activity, Category: amides-buliding-blocks, the publication is Journal of Medicinal Chemistry (2009), 52(9), 2673-2682, database is CAplus and MEDLINE.

The tenovins and cambinol are two classes of sirtuin inhibitor that exhibit antitumor activity in preclin. models. This report describes modifications to the core structure of cambinol, in particular by incorporation of substituents at the N1-position, which lead to increased potency and modified selectivity. These improvements have been rationalized using mol. modeling techniques. The expected functional selectivity in cells was also observed for both a SIRT1 and a SIRT2 selective analog.

Journal of Medicinal Chemistry 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, Category: amides-buliding-blocks.

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

James, Carrie R. published the artcilePoly(oligonucleotide), Computed Properties of 186046-83-3, the publication is Journal of the American Chemical Society (2014), 136(32), 11216-11219, database is CAplus and MEDLINE.

Here we report the preparation of poly(oligonucleotide) brush polymers and amphiphilic brush copolymers from nucleic acid monomers via graft-through polymerization We describe the polymerization of PNA-norbornyl monomers to yield poly-PNA (poly(peptide nucleic acid)) via ring-opening metathesis polymerization (ROMP) with the initiator, (IMesH₂)(C₅H₅N)₂(Cl)₂RuCHPh. In addition, we present the preparation of poly-PNA nanoparticles from amphiphilic block copolymers and describe their hybridization to a complementary single-stranded DNA (ssDNA) oligonucleotide.

Journal of the American Chemical Society 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 C40H35N7O8, Computed Properties of 186046-83-3.

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

Pinto, Brunella published the artcileSynthesis and label free characterization of a bimolecular PNA homo quadruplex, Formula: C40H35N7O8, the publication is Biochimica et Biophysica Acta, General Subjects (2017), 1861(5_Part_B), 1222-1228, database is CAplus and MEDLINE.

G-quadruplex DNA is involved in many physiol. and pathol. processes. Both clin. and exptl. studies on DNA G-quadruplexes are slowed down by their enzymic instability. In this frame, more stable chem. modified analogs are needed. The bis-end-linked-(gggt)₂ PNA mol. (BEL-PNA) was synthesized using in solution and solid phase synthetic approaches. Quadruplex formation was assessed by CD (CD) and surface enhanced Raman scattering (SERS). An unprecedented bimol. PNA homo quadruplex is here reported. To achieve this goal, we developed a bifunctional linker that once functionalized with gggt PNA strands and annealed in K⁺ buffer allowed the obtainment of a PNA homo quadruplex. 4The identification of the strong SERS band at ∼ 1481 cm^– 1, attributable to vibrations involving the quadruplex diagnostic Hoogsteen type hydrogen bonds, confirmed the formation of the PNA homo quadruplex. By tethering two G-rich PNA strands to the two ends of a suitable bifunctional linker it is possible to obtain bimol. PNA homo quadruplexes after annealing in K⁺-containing buffers. The formation of such CD-unfriendly complexes can be monitored, even at low concentrations, by using the SERS technique. Given the importance of DNA G-quadruplexes in medicine and nanotechnol., the obtainment of G-quadruplex analogs provided with enhanced enzymic stability, and their monitoring by highly sensitive label-free techniques are of the highest importance. This article is part of a Special Issue entitled “G-quadruplex” – guest edited by Dr. Concetta Giancola and Dr. Daniela Montesarchio.

Biochimica et Biophysica Acta, General Subjects 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 C40H35N7O8, Formula: C40H35N7O8.

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

Bakunov, Stanislav A. published the artcileModification of the Tiemann rearrangement: One-pot synthesis of N,N-disubstituted cyanamides from amidoximes, SDS of cas: 2451-91-4, the publication is Synthesis (2000), 1148-1159, database is CAplus.

Amidoximes were converted to N,N-disubstituted cyanamides in 70-92% yield in a one-pot synthetic procedure by treating the amidoximes with tosyl chloride, followed by treatment with alkyl halide under phase-transfer conditions.

Synthesis published new progress about 2451-91-4. 2451-91-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Benzene, name is N,N-Dibenzylcyanamide, and the molecular formula is C15H14N2, SDS of cas: 2451-91-4.

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

Jack, Thomas published the artcileSynthesis and characterization of photoaffinity probes that target the 5-HT₃ receptor, Application of N,N-Diethyl-2,2,2-trifluoroacetamide, the publication is Chimia (2014), 68(4), 239-242, database is CAplus and MEDLINE.

The 5-HT₃ receptor is one of several ion channels responsible for the transmission of nerve impulses in the peripheral and central nervous systems. Until now, it was difficult to characterize transmembrane receptors with classical structural biol. approaches like x-ray crystallog. The use of photoaffinity probes is an alternative approach to identify regions in the protein where small mols. bind. To this end, the authors present two photoaffinity probes based on granisetron, a well known antagonist of the 5-HT₃ receptor. These new probes show nanomolar binding affinity for the orthosteric binding site. In addition, the authors investigated their reactivity using irradiation experiments

Chimia published new progress about 360-92-9. 360-92-9 belongs to amides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Amine,Aliphatic hydrocarbon chain,Amide, name is N,N-Diethyl-2,2,2-trifluoroacetamide, and the molecular formula is C6H10F3NO, Application of N,N-Diethyl-2,2,2-trifluoroacetamide.

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