Wilking, Melissa J.’s team published research in Archives of Biochemistry and Biophysics in 563 | CAS: 380315-80-0

Archives of Biochemistry and Biophysics 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 C9H10ClNO2, SDS of cas: 380315-80-0.

Wilking, Melissa J. published the artcileSIRT1 deacetylase is overexpressed in human melanoma and its small molecule inhibition imparts anti-proliferative response via p53 activation, SDS of cas: 380315-80-0, the publication is Archives of Biochemistry and Biophysics (2014), 94-100, database is CAplus and MEDLINE.

Melanoma causes more deaths than any other skin cancer, and its incidence in the US continues to rise. Current medical therapies are insufficient to control this deadly neoplasm, necessitating the development of new target-based approaches. The objective of this study was to determine the role and functional significance of the class III histone deacetylase SIRT1 in melanoma. We have found that SIRT1 is overexpressed in clin. human melanoma tissues and human melanoma cell lines (Sk-Mel-2, WM35, G361, A375, and Hs294T) compared to normal skin and normal melanocytes, resp. In addition, treatment of melanoma cell lines A375, Hs294T, and G361 with Tenovin-1, a small mol. SIRT1 inhibitor, resulted in a significant decrease in cell growth and cell viability. Further, Tenovin-1 treatment also resulted in a marked decrease in the clonogenic survival of melanoma cells. Further experiments showed that the anti-proliferative response of Tenovin-1 was accompanied by an increase in the protein as well as activity of the tumor suppressor p53. This increase in p53 activity was substantiated by an increase in the protein level of its downstream target p21. Overall, these data suggest that small mol. inhibition of SIRT1 causes anti-proliferative effects in melanoma cells. SIRT1 appears to be acting through the activity of the tumor suppressor p53, which is not mutated in the majority of melanomas. However, future detailed studies are needed to further explore the role and mechanism of SIRT1 in melanoma development and progression and its usefulness in melanoma treatment.

Archives of Biochemistry and Biophysics 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 C9H10ClNO2, SDS of cas: 380315-80-0.

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

Monty, Olivier B. C.’s team published research in ACS Combinatorial Science in 22 | CAS: 2418-95-3

ACS Combinatorial Science 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.

Monty, Olivier B. C. published the artcileSolution-phase fmoc-based peptide synthesis for DNA-encoded chemical libraries: Reaction conditions, protecting group strategies, and pitfalls, Recommanded Product: H-Lys(Boc)-OH, the publication is ACS Combinatorial Science (2020), 22(12), 833-843, database is CAplus and MEDLINE.

Peptide drug discovery has shown a resurgence since 2000, bringing 28 non-insulin therapeutics to the market compared to 56 since its first peptide drug, insulin, in 1923. While the main method of discovery has been biol. display-phage, mRNA, and ribosome-the synthetic limitations of biol. systems has restricted the depth of exploration of peptide chem. space. In contrast, DNA-encoded chem. offers the synergy of large numbers and ribosome-independent synthetic flexibility for the fast and deeper exploration of the same space. Hence, as a bridge to building DNA-encoded chem. libraries (DECLs) of peptides, we have developed substrate-tolerant amide coupling reaction conditions for amino acid monomers, performed a coupling screen to illustrate such tolerance, developed protecting group strategies for relevant amino acids and reported the limitations thereof, developed a strategy for the coupling of α,α-disubstituted alkenyl amino acids relevant to all-hydrocarbon stapled peptide drug discovery, developed reaction conditions for the coupling of tripeptides likely to be used in DECL builds, and synthesized a fully deprotected DNA-decamer conjugate to illustrate the potency of the developed methodol. for on-DNA peptide synthesis.

ACS Combinatorial Science 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

Madadian, Edris’s team published research in Chemosphere in 303 | CAS: 137862-53-4

Chemosphere published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Quality Control of 137862-53-4.

Madadian, Edris published the artcileThermal degradation of emerging contaminants in municipal biosolids: The case of pharmaceuticals and personal care products, Quality Control of 137862-53-4, the publication is Chemosphere (2022), 303(Part_2), 135008, database is CAplus and MEDLINE.

The presence of emerging contaminants in water and wastewater resources is of ongoing concern for public health and safety. Pharmaceutical compounds are designed to be biol. active and therefore may have effects on nontarget organisms in terrestrial and aquatic environments, even at trace concentrations The presence of pharmaceutical and personal care products (PPCPs) in wastewater treatment plants is reported in various countries worldwide, mostly in the levels of nanograms to micrograms per L. The present study investigates the thermal degradation of municipal sewage sludge containing PPCPs at various heating rates. The examined characteristics of the samples include thermal decomposition behavior, volatile release characteristics, and pyrolytic product composition Thermal characterization of the PPCPs was conducted using differential scanning calorimetry. The gaseous products and typical functional groups of the released volatiles detected by Fourier-transform IR spectroscopy mainly contained CO2, CO, small-chain hydrocarbons, and oxygen- and nitrogen-containing functional groups together with other species. In addition, the potential of bioenergy production was investigated as a spin-off opportunity during thermal degradation of biosolids. Study results showed that PPCP concentrations can be lowered significantly by thermal treatment of municipal biosolids. Antifungal/antibacterial agents together with opioids, in particular triclosan and tramadol, showed less resistance to thermal degradation while antibiotics could be more recalcitrant to heat treatment. The thermodn. results provide an important reference for future reactor design and the thermochem. treatment of biosolids as well as their conversion to value-added products.

Chemosphere published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Quality Control of 137862-53-4.

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

Dettin, Monica’s team published research in Molecules in 17 | CAS: 186046-83-3

Molecules 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, Recommanded Product: 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.

Dettin, Monica published the artcileSynthesis and chromatography-free purification of PNA-PEO conjugates for the functionalisation of gold sensors, Recommanded Product: 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, the publication is Molecules (2012), 11026-11045, database is CAplus and MEDLINE.

Peptide Nucleic Acids (PNAs) linked to high mol. weight (MW) poly(ethylene oxide) (PEO) derivatives could be useful conjugates for the direct functionalisation of gold surfaces dedicated to Surface Plasmon Resonance (SPR)-based DNA sensing. However their use is hampered by the difficulty to obtain them through a convenient and economical route. In this work we compared three synthetic strategies to obtain PNA-high MW PEO conjugates composed of (a) a 15-mer PNA sequence as the probe complementary to genomic DNA of Mycobacterium tuberculosis, (b) a PEO moiety (2 or 5 KDa MW) and (c) a terminal trityl-protected thiol necessary (after acidic deprotection) for grafting to gold surfaces. The 15-mer PNA was obtained by solid-phase synthesis. Its amino terminal group was later condensed to bi-functional PEO derivatives (2 and 5 KDa MW) carrying a Trt-cysteine at one end and a carboxyl group at the other end. The reaction was carried out either in solution, using HATU or PyOxim as coupling agents or through the solid-phase approach, with 49.6%, 100% and 5.2% yield, resp. A differential solvent extraction strategy for product purification without the need for chromatog. is described. The ability of the 5 KDa PEO conjugate to function as a probe for complementary DNA detection was demonstrated using a Grating-Coupling Surface Plasmon Resonance (GC-SPR) system. The optimized PEO conjugation and purification protocols are economical and simple enough to be reproduced also within laboratories that are not highly equipped for chem. synthesis.

Molecules 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, Recommanded Product: 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.

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

Xu, Liang’s team published research in Tetrahedron in 62 | CAS: 489-17-8

Tetrahedron published new progress about 489-17-8. 489-17-8 belongs to amides-buliding-blocks, auxiliary class Fluoride,Sulfamide,Amine,Benzene, name is 4-Fluoro-2-methylbenzenesulfonamide, and the molecular formula is C17H20ClN3, Application of 4-Fluoro-2-methylbenzenesulfonamide.

Xu, Liang published the artcileOxidative cyclization of N-alkyl-o-methyl-arenesulfonamides to biologically important saccharin derivatives, Application of 4-Fluoro-2-methylbenzenesulfonamide, the publication is Tetrahedron (2006), 62(33), 7902-7910, database is CAplus.

Various biol. important saccharin skeletons and their N-alkyl derivatives were efficiently prepared by Cr(VI) oxide-catalyzed H5IO6 oxidation of N-alkyl-o-methyl-arenesulfonamides in MeCN. N-tert-Bu saccharin skeletons were easily prepared by H5IO6-CrO3 oxidation of N-tert-butyl-o-Me arenesulfonamides in the presence of acetic anhydride. The method that furnished the novel fluoro- and trifluoromethyl-substituted saccharin skeletons was characterized by two steps, a simple work-up procedure, a single purification and good overall yields from substituted toluene derivatives For example, 58 % 2-tert-butyl-6-trifluoromethyl-1,2-benzisothiazol-3-one 1,1-dioxide was obtained from 1-methyl-4-(trifluoromethyl)benzene.

Tetrahedron published new progress about 489-17-8. 489-17-8 belongs to amides-buliding-blocks, auxiliary class Fluoride,Sulfamide,Amine,Benzene, name is 4-Fluoro-2-methylbenzenesulfonamide, and the molecular formula is C17H20ClN3, Application of 4-Fluoro-2-methylbenzenesulfonamide.

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

Devani, M. B.’s team published research in Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry in 14B | CAS: 15029-36-4

Indian Journal of Chemistry, Section B: Organic Chemistry Including 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, Safety of 2-Cyano-N-ethylacetamide.

Devani, M. B. published the artcileSynthesis of 2-aminothiophenes and thieno[2,3-d]pyrimidines, Safety of 2-Cyano-N-ethylacetamide, the publication is Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry (1976), 14B(5), 357-60, database is CAplus.

The thienopyrimidinones I [R = Me, R1 = CO2Et, R2 = H; RR1 = (CH2)4, R2 = Ph] were prepared by treating the aminothiophenes II (R = CO2Et, CONHPh) with HCONH2 or (EtO)3CH, whereas cyclization of II [R = Me, R1 = EtO2C, R3 = cyano; RR1 = (CH2)4, R3 = cyano] with HCONH2 gave the corresponding aminothienopyrimidines III. Furthermore, the spiro[benzothienopyrimidine-2,1′-cyclohexane] IV was prepared by cyclization of NCCH2CONHNHPh with cyclohexanone in the presence of S. IV had antiinflammatory and anticonvulsant activities and II had only antiinflammatory activity.

Indian Journal of Chemistry, Section B: Organic Chemistry Including 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, Safety of 2-Cyano-N-ethylacetamide.

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

Devani, M. B.’s team published research in Arzneimittel-Forschung in 27 | CAS: 15029-36-4

Arzneimittel-Forschung 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.

Devani, M. B. published the artcileSynthesis and pharmacological properties of some 4-amino-5-substituted thiazole-2(3H)-thiones and thiazolo(4,5-d)pyrimidin-7(6H)-one-2(3H)-thiones, Recommanded Product: 2-Cyano-N-ethylacetamide, the publication is Arzneimittel-Forschung (1977), 27(9), 1652-5, database is CAplus and MEDLINE.

Twenty-six aminothiazolethiones I (R = Et, benzyl, allyl, Ph, tolyl, etc.; R1 = NH2, NHMe, piperidino, morpholino, PhNHNH) were prepared in 40-90% yield by reaction of RNCS with NCCH2CONHR1. Eleven thiazolopyrimidinones II (R = benzyl, tolyl, Ph, Me, Et, R2 = H, Me, Et, Ph, anilino) were prepared in 55-70% yield by reaction of the appropriate I with HC(OEt)2 in Ac2O. I and II were screened for antimicrobial and pharmacol. activities. Maximum antiinflammatory activity was found in I (R = o-tolyl, R1 = morpholino); at 200 mg/kg its activity was almost equal to phenylbutazone at 100 mg/kg. I (R = allyl, R1 = PhNHNH) was the most active antimicrobial of the series. I (R = benzyl, R1 = NH2) was the most potent analgesic.

Arzneimittel-Forschung 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

Shimbori, Chiko’s team published research in Experimental Lung Research in 36 | CAS: 321673-30-7

Experimental Lung 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 C8H11BO2, Application of [(2-Hexylcyclopentylidene)amino]thiourea.

Shimbori, Chiko published the artcileInvolvement of leukotrienes in the pathogenesis of silica-induced pulmonary fibrosis in mice, Application of [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Experimental Lung Research (2010), 36(5), 292-301, database is CAplus and MEDLINE.

The authors investigated the role of leukotrienes (LTs) in the pathogenesis of silica-induced pulmonary fibrosis in mice during the progression from acute to chronic phases. Intratracheal instillation of silica particles induced progressive pulmonary fibrosis. The tissue content of cysteinyl (Cys) LTs and LTB4 was markedly increased in the acute phase after silica instillation, concurrently with the up-regulation of LTB4 receptor, transforming growth factor (TGF)-β1, and tumor necrosis factor (TNF)-α, along with down-regulation of the CysLT type 2 receptor. Importantly, the tissue content of CysLTs and mRNA levels of TGF-β1 and TNF-α were increased in the fibrotic lung in the chronic phase. Furthermore, strong immunohistochem. staining for the CysLT type 1 receptor, TNF-α, and TGF-β1, but not for the CysLT type 2 receptor, was codetected in the pathol. lesions during both acute and chronic phases. These findings suggest that an increase in LT production in the lung and modulation of homeostatic balance among LT receptors may contribute to the progression of pulmonary fibrosis.

Experimental Lung 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 C8H11BO2, Application of [(2-Hexylcyclopentylidene)amino]thiourea.

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

Suzuki, Hirotsugu’s team published research in Organic & Biomolecular Chemistry in 18 | CAS: 100377-32-0

Organic & Biomolecular Chemistry published new progress about 100377-32-0. 100377-32-0 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N-Methoxy-N-methylisonicotinamide, and the molecular formula is C9H9BrO2, Synthetic Route of 100377-32-0.

Suzuki, Hirotsugu published the artcileDealkoxylation of N-alkoxyamides without an external reductant driven by Pd/Al cooperative catalysis, Synthetic Route of 100377-32-0, the publication is Organic & Biomolecular Chemistry (2020), 18(38), 7545-7548, database is CAplus and MEDLINE.

Lewis acid-assisted palladium-catalyzed dealkoxylation of N-alkoxyamides has been developed. This reaction proceeded smoothly with a range of N-alkoxyamides in the absence of an external reductant, thereby establishing a convenient and reductant-free protocol. In addition, a gram-scale reaction could be achieved. Preliminary mechanistic investigations indicated that β-hydrogen elimination from a palladium alkoxide intermediate generated an intramol. hydride source.

Organic & Biomolecular Chemistry published new progress about 100377-32-0. 100377-32-0 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N-Methoxy-N-methylisonicotinamide, and the molecular formula is C9H9BrO2, Synthetic Route of 100377-32-0.

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

Rossi, Steven A.’s team published research in Organic Letters in 15 | CAS: 2447-79-2

Organic Letters published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, Category: amides-buliding-blocks.

Rossi, Steven A. published the artcileSelective Formation of Secondary Amides via the Copper-Catalyzed Cross-Coupling of Alkylboronic Acids with Primary Amides, Category: amides-buliding-blocks, the publication is Organic Letters (2013), 15(9), 2314-2317, database is CAplus and MEDLINE.

For the first time, a general catalytic procedure for the cross-coupling of primary amides and alkylboronic acids is demonstrated. The key to the success of this reaction was the identification of a mild base (NaOSiMe3) and oxidant (di-tert-Bu peroxide) to promote the copper-catalyzed reaction in high yield. This transformation provides a facile, high-yielding method for the monoalkylation of amides.

Organic Letters published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, Category: amides-buliding-blocks.

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