Month: November 2022

Singh, Chandra K published the artcileNovel downstream molecular targets of SIRT1 in melanoma: a quantitative proteomics approach., Computed Properties of 380315-80-0, the publication is Oncotarget (2014), 5(7), 1987-99, database is MEDLINE.

Melanoma is one of the most lethal forms of skin cancer and its incidence is continuing to rise in the United States. Therefore, novel mechanism and target-based strategies are needed for the management of this disease. SIRT1, a NAD(+)-dependent class III histone deacetylase, has been implicated in a variety of physiological processes and pathological conditions. We recently demonstrated that SIRT1 is upregulated in melanoma and its inhibition by a small-molecule, tenovin-1, inhibits cell proliferation and clonogenic survival of melanoma cells, possibly via activating p53. Here, we employed a gel free quantitative proteomics approach to identify the downstream effectors and targets of SIRT1 in melanoma. The human malignant melanoma, G361 cells were treated with tenovin-1 followed by protein extraction, in liquid trypsin digestion, and peptide analyses using nanoLC-MS/MS. A total of 1091 proteins were identified, of which 20 proteins showed significant differential expression with 95% confidence interval. These proteins were subjected to gene ontology and Ingenuity Pathway Analysis (IPA) to obtain the information regarding their biological and molecular functions. Real-Time qRT-PCR validation showed that five of these (PSAP, MYO1B, MOCOS, HIS1H4A and BUB3) were differentially expressed at mRNA levels. Based on their important role in cell cycle regulation, we selected to focus on BUB family proteins (BUB3, as well as BUB1 and BUBR1) for subsequent validation. The qRT-PCR and immunoblot analyses showed that tenovin-1 inhibition of SIRT1 resulted in a downregulation of BUB3, BUB1 and BUBR1 in multiple melanoma cell lines. Since tenovin-1 is an inhibitor of both SIRT1 and SIRT2, we employed lentivirus mediated silencing of SIRT1 and SIRT2 in G361 cells to determine if the observed effects on BUB family proteins are due to SIRT1- or SIRT2- inhibition. We found that only SIRT1 inhibition resulted in a decrease in BUB3, BUB1 and BUBR1. Our study identified the mitotic checkpoint regulator BUB family proteins as novel downstream targets of SIRT1. However, further validation is needed in appropriate models to confirm our findings and expand on our observations.

Oncotarget published new progress about 380315-80-0. 380315-80-0 belongs to amides-buliding-blocks, auxiliary class Apoptosis,p53, name is N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide, and the molecular formula is C10H6F17N, Computed Properties of 380315-80-0.

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

Adel M. Kamal El-Dean published the artcileNovel Synthesis, Reactions, and Biological Study of New Morpholino-Thieno[2,3-c][2,7]Naphthyridines as Anti-Cancer and Anti-Microbial Agents, COA of Formula: C2H4ClNO, the publication is Russian Journal of Bioorganic Chemistry, database is CAplus.

The biol. uses of 2,7-naphthyridines have sparked great attention in recent years. For this reason, a series of novel 2,7-naphthyridines derivatives was synthesized and explored their spectrum and biol. properties in this study. Compound I was prepared by the reaction of 1-Me piperidin-4-one with CS₂, malononitrile, and triethylamine. The condensed I be converted to II by reaction with morpholine. Composite II was used as a starter in heterocyclic compound a series, such as the thieno[2,3-c][2,7]naphthyridines III (R = CN, COOEt, COPh, etc.). Authors used III (R = COOEt), III (R = CONH₂) and III (R = CHO) as a precursor to create original heterocyclic moieties, namely: pyrimidothienonaphthyridino and pyridothieno naphthyridino in compounds A number of compounds for antimicrobial activity were examined against a variety of bacterial and fungal strains. In addition, some of these compounds showed anticancer activity in liver and cells of breast cancer.

Russian Journal of Bioorganic Chemistry 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, COA of Formula: C2H4ClNO.

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

Davis, H. Lorne published the artcile2,3-Disubstituted 1,8-naphthyridines as potential diuretic agents. 3. 4- and 7-Phenyl derivatives, Recommanded Product: 2-Cyano-N-ethylacetamide, the publication is European Journal of Medicinal Chemistry (1985), 20(4), 381-3, database is CAplus.

Naphthyridines I [R = Ph, OH, NH₂; R¹ = cyano, (un)substituted CONH₂, CO₂Me; R², R³ = H, Ph] were prepared Thus, 2-amino-3-benzoylpyridine (II) was cyclized with NCCH₂CONH₂ to give I (R = OH, R¹ = cyano, R² = Ph, R³ = H) (III). Cyclocondensation of II and CH₂(CN)₂ gave I (R = NH₂; R¹ = cyano, R² = Ph, R³ = H), which was hydrolyzed to I (R¹ = CONH₂) (IV). III and IV were as potent diuretics as triamterene, but I (R³ = Ph) were inactive.

European Journal of Medicinal Chemistry 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, Recommanded Product: 2-Cyano-N-ethylacetamide.

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

Hao, Jiamao published the artcileHighly regioselective Ru(II)-catalyzed [3+2] spiroannulation of 1-aryl-2-naphthols with alkynes via a double directing group strategy, Related Products of amides-buliding-blocks, the publication is Tetrahedron Letters (2021), 153050, database is CAplus.

A highly regioselective Ru(II)-catalyzed [3+2] spiroannulation of 1-aryl-2-naphthols with internal alkynes was developed by using a novel double directing group strategy. This method was compatible with many functional groups, thus affording a variety of sterically congested spirocyclic mols. in high yields.

Tetrahedron Letters published new progress about 1197171-76-8. 1197171-76-8 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronate Esters,Boronic Acids,Boronic acid and ester,, name is N-Methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide, and the molecular formula is C14H20BNO3, Related Products of amides-buliding-blocks.

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

Bruyat, Pierrick published the artcileUse of an air-stable Cu(I)-NHC catalyst for the synthesis of peptidotriazoles, Category: amides-buliding-blocks, the publication is Journal of Organic Chemistry (2018), 83(21), 13515-13522, database is CAplus and MEDLINE.

We report the use of air-stable Cu(I)-NHC complex 4a as a catalyst for the efficient microwave-assisted synthesis of peptidotriazoles on solid phase. Compared with the usual conditions (CuI or CuSO₄/NaAsc), catalyst (I) allowed the preparation of a series of peptidomimetic compounds containing a 1,2,3-triazole ring in their backbone without the oxidation of common side-chains. Overall, the peptidotriazoles were obtained in good yields (61-87%), in excellent purity (higher than 94%) and with low copper contamination.

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

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

Pipalde, Amrit Kumar published the artcileStudies on chemical mediated induction of resistance in chickpea against dry root rot (Rhizoctonia bataticola), Related Products of amides-buliding-blocks, the publication is Pharma Innovation (2021), 10(7), 1068-1073, database is CAplus.

The present research work on, “Investigations on chem. mediated induction of resistance in chickpea against dry root rot (Rhizoctonia bataticola).” was carried out in the Section of Plant Pathol., College of Agriculture, Indore, during 2011-12 using variety JG-62. The object of the present investigation were evaluation of SAR inducing chems. against Rhizoctonia bataticola in vitro, evaluation of SAR inducing chems. for control of dry root rot in poly house and for control of dry root rot in the field at different concentrations The experiments were conducted with nine treatments in a Randomized Block Design with three replications and Completely Randomized Design with four replications; observations were recorded at different days after sowing. The typical symptoms of the disease and characterization of the pathogen were described to identify it as R. bataticola. Studies on control of dry root rot by seed treatments and foliar application of SAR compounds were undertaken. Among the tested treatments salicylic acid at 400ppm applied as seed treatment along with its foliar application at 30 DAS and seed treatment with 200ppm isonicotinamide and foliar application of isonicotinamide with 200ppm at 30 DAS were most effective. Seed treatments with 200ppm salicylic acid with 200ppm isonicotinamide was the least effective treatment against R. bataticola. Experiments carried out to evaluate the resistance through salicylic acid and isonicotinamide reduced disease incidence caused by R. bataticola by imparting resistance to the host rather than directly affecting the pathogen. Studies on effect of seed treatments and foliar application on the incidence of dry root rot in chickpea showed that the disease incidence was significantly reduced by combination seed treatment with 400ppm salicylic acid and foliar application of salicylic acid with 400ppm at 30 DAS and seed treatment with 200ppm isonicotinamide and foliar application of isonicotinamide with 200ppm at 30 DAS. But salicylic acid at 400ppm applied as seed treatment along with its foliar application at 30 DAS proved as the best with respect to other control measures.

Pharma Innovation published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Related Products of amides-buliding-blocks.

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

Sosniak, Anna M. published the artcileThermal melting studies of alkyne- and ferrocene-containing PNA bioconjugates, Related Products of amides-buliding-blocks, the publication is Organic & Biomolecular Chemistry (2009), 7(23), 4992-5000, database is CAplus and MEDLINE.

The preparation of new metal-containing peptide nucleic acids (PNAs) is currently a field of research intensively studied for various purposes, such as DNA biosensors. The role played by the metal center, notably on the stability of the PNA·DNA hybrid, is obviously crucial, but has not yet been fully investigated. In this work, UV-Vis spectroscopic measurements of solutions of DNA·PNA hybrids, whose 11/12-mer PNA oligomers contained either alkynyl PNA monomer I or ferrocene-containing PNA monomer II, were carried out to determine the effect of these monomers on the thermal stability of the hybrids (PNA = H-Gly-X-gggtc-Y-agctt-X-Lys-NH₂; X, Y = I, II, blank position). Supplementary CD spectroscopic measurements were performed to gain insight into the structures of the PNA·DNA duplexes formed. The effect of both modified monomers was found to depend on their actual positions within the PNA sequences. Insertions at the N- or C-termini of a PNA oligomer did not change the melting temperatures (T_m values of about 72°) of the DNA·PNA hybrids significantly. Insertion of monomers I or II in the middle of a PNA sequence induced a substantial decrease in the T_m of the hybrids (by about 23°) when bound to the same DNA oligomer. Interestingly, it was found that the type of modification, namely alkyne or ferrocene, did not significantly influence the T_m values in these cases. However, the thermal stability of hybrids with the DNA oligomers containing one to four addnl. thymines and the PNA oligomers containing the ferrocene moiety in its middle, varied significantly with the number of thymines added compared to its alkyne analogs (ΔT_m up to -13°). The presence of the ferrocene moiety induced a significant decrease in thermal stability of the hybrids, probably due to its bulkiness. In order to assess the effect of PNA backbone rigidity on the stability of DNA·PNA hybrids, PNA oligomers with an internal amino acid, propargylglycine (Pgl) or the dipeptide glycine-propargylglycine (Gly-Pgl), were synthesized. It was assumed that the orientation of the alkyne moiety in the Pgl-containing PNA sequence is not identical to an alkyne-containing PNA sequence, as a significantly higher T_m value (ΔT_m = +10°) was measured. It is anticipated that the alkyne moiety in Pgl is not facing the DNA base and therefore does not disturb as much the neighboring nucleobases and base-stacking of the complementary DNA, in contrast to the alkyne moiety of I. Interestingly, no significant differences in the thermal stability of the hybrids was observed between Pgl-containing and dipeptide-containing PNA oligomers, although the former contracts the PNA backbone by three atoms.

Organic & Biomolecular 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 C6H16OSi, Related Products of amides-buliding-blocks.

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

Husken, Nina published the artcile“Four-Potential” Ferrocene Labeling of PNA Oligomers via Click Chemistry, Category: amides-buliding-blocks, the publication is Bioconjugate Chemistry (2009), 20(8), 1578-1586, database is CAplus and MEDLINE.

The scope of the Cu(I)-catalyzed [2 + 3] azide/alkyne cycloaddition (CuAAC, click chem.) as a key reaction for the conjugation of ferrocene derivatives to N-terminal functionalized PNA oligomers is explored herein (PNA: peptide nucleic acid). The facile solid-phase synthesis of N-terminal azide or alkyne-functionalized PNA oligomer precursors and their cycloaddition with azidoferrocene, ethynylferrocene, and N-(3-ethylpent-1-yn-3-yl)ferrocene-carboxamide (DEPA-ferrocene) on the solid phase are presented. While the click reaction with azidomethylferrocene worked equally well, the ferrocenylmethyl group is lost from the conjugate upon acid cleavage. However, the desired product was obtained via a post-SPPS conversion of the alkyne-PNA oligomer with azidomethylferrocene in solution The synthesis of all ferrocene-PNA conjugates (trimer t₃-PNA, 3, 4, 5, 6; 12mer PNA, 10 – t c t a c a a g a c t c, 11 – t c t a c c g t a c t c) succeeded with excellent yields and purities, as determined by mass spectrometry and HPLC. Electrochem. studies of the trimer Fc-PNA conjugates 3, 4, 5, and 6 with four different ferrocene moieties revealed quasi-reversible redox processes of the ferrocenyl redox couple Fc^0/+ and electrochem. half-wave potentials in a range of E_1/2 = -20 mV to +270 mV vs FcH^0/+ (Fc: ferrocenyl, C₁₀H₉Fe). The observed potential differences ΔE_1/2^min are always greater than 60 mV for any given pair of Fc-PNA conjugates, thus allowing a reliable differentiation with sensitive electrochem. methods like e.g. square wave voltammetry (SWV). This is the electrochem. equivalent of “four-color” detection and is hence denoted “four-potential” labeling. Preparation and electrochem. investigation of the set of four structurally different and electrochem. distinguishable ferrocenyl groups conjugated to PNA oligomers, as exemplified by the conjugates 3, 4, 5, and 6, demonstrates the scope of the azide/alkyne cycloaddition for the labeling of PNA with electrochem. active ferrocenyl groups. Furthermore, it provides a PNA-based system for the electrochem. detection of single-nucleotide polymorphism (SNP) in DNA/RNA.

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 C40H35N7O8, Category: amides-buliding-blocks.

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

Waisser, K. published the artcileHydrophobic properties of some thiobenzamides, antimycobacterially active compounds, Category: amides-buliding-blocks, the publication is Folia Pharmaceutica Universitatis Carolinae (1998), 23(Suppl.), 114-115, database is CAplus.

HPLC was used to assess the hydrophobic properties of 11 PhCSNH₂ (R = H, 3- and 4-MeO and -Cl, 4-O₂N, 4-Me₂N, 4-Me, 4-MeS, 3,4-Cl₂, 3-Br). A correlation equation was derived for this series of compounds, based on hydrophobic substituent constants calculated for R.

Folia Pharmaceutica Universitatis Carolinae 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 C11H12O4, Category: amides-buliding-blocks.

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

Gutierrez-Seijo, Alba published the artcileActivin A Sustains the Metastatic Phenotype of Tumor-Associated Macrophages and Is a Prognostic Marker in Human Cutaneous Melanoma, Category: amides-buliding-blocks, the publication is Journal of Investigative Dermatology (2022), 142(3_Part_A), 653-661.e2, database is CAplus and MEDLINE.

Tumor cells attract and dynamically interact with monocytes/macrophages to subvert their differentiation into tumor-associated macrophages (TAMs), which mainly promote immune suppression and neoplastic progression, but the pathways and microenvironmental cues governing their protumoral deviation are not completely understood. To identify the mol. pathways responsible for TAM differentiation, we screened the biomarkers secreted during melanoma-macrophage interactions using Quantibody microarrays and RNA sequencing of macrophages. We found that activin A, a member of the transforming GF family, plays an instrumental role in the cross-talk between melanoma cells and monocytes/macrophages, which results in the upregulation of distinct tumor-sustaining genes and the achievement of proinvasive and immunosuppressive functions of TAMs. Blockade of activin reduces the upregulation of part of these genes and prevents the acquisition of protumoral functions, facilitating human melanoma rejection by transferred human lymphocytes in a xenograft mouse model. Remarkably, screening of two independent cutaneous primary melanoma collections showed that activin A is enriched in TAMs and melanoma cells from patients with worse outcomes and constitutes a new and independent prognostic marker. Thus, we identify activin A as a key intermediary in the protumoral and immunosuppressive functions of TAMs, with significant potential as a disease biomarker as well as an immunotherapeutic target.

Journal of Investigative Dermatology 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, Category: amides-buliding-blocks.

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