Month: December 2022

Boschelli, Diane H. published the artcileSynthesis and Src kinase inhibitory activity of a series of 4-phenylamino-3-quinolinecarbonitriles, HPLC of Formula: 2447-79-2, the publication is Journal of Medicinal Chemistry (2001), 44(5), 822-833, database is CAplus and MEDLINE.

Screening of a directed compound library in a yeast-based assay identified 4-[(2,4-dichlorophenyl)amino]-6,7-dimethoxy-3-quinolinecarbonitrile (I) as a Src inhibitor. An enzymic assay established that I was an ATP-competitive inhibitor of the kinase activity of Src. We present here SAR data for I which shows that the aniline group at C-4, the carbonitrile group at C-3, and the alkoxy groups at C-6 and C-7 of the quinoline are crucial for optimal activity. Increasing the size of the C-2 substituent of the aniline at C-4 of I from chloro to bromo to iodo resulted in a corresponding increase in Src inhibition. Furthermore, replacement of the 7-methoxy group of I with various 3-heteroalkylaminopropoxy groups provided increased inhibition of both Src enzymic and cellular activity. Compound II, which contains a 3-morpholinopropoxy group, had an IC₅₀ of 3.8 nM in the Src enzymic assay and an IC₅₀ of 940 nM for the inhibition of Src-dependent cell proliferation.

Journal of Medicinal Chemistry 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, HPLC of Formula: 2447-79-2.

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

Lei, Yiting published the artcileShear-responsive boundary-lubricated hydrogels attenuate osteoarthritis, SDS of cas: 169590-42-5, the publication is Bioactive Materials (2022), 472-484, database is CAplus and MEDLINE.

Lipid-based boundary layers formed on liposome-containing hydrogels can facilitate lubrication. However, these boundary layers can be damaged by shear, resulting in decreased lubrication. Here, a shear-responsive boundary-lubricated drug-loaded hydrogel is created by incorporating celecoxib (CLX)-loaded liposomes within dynamic covalent bond-based hyaluronic acid (HA) hydrogels (CLX@Lipo@HA-gel). The dynamic cross-linked network enables the hydrogel to get restructured in response to shear, and the HA matrix allows the accumulation of internal liposome microreservoirs on the sliding surfaces, which results in the formation of boundary layers to provide stable lubrication. Moreover, hydration shells formed surrounding the hydrogel can retard the degradation process, thus helping in sustaining lubrication. Furthermore, in vitro and in vivo experiments found that CLX@Lipo@HA-gels can maintain anabolic-catabolic balance, alleviate cartilage wear, and attenuate osteoarthritis progression by delivering CLX and shear-responsive boundary lubrication. Overall, CLX@Lipo@HA-gels can serve as shear-responsive boundary lubricants and drug-delivery vehicles to alleviate friction-related diseases like osteoarthritis.

Bioactive Materials 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, SDS of cas: 169590-42-5.

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

He, Haifeng published the artcileSynthesis, antitumor activity and mechanism of action of novel 1,3-thiazole derivatives containing hydrazide-hydrazone and carboxamide moiety, SDS of cas: 2447-79-2, the publication is Bioorganic & Medicinal Chemistry Letters (2016), 26(14), 3263-3270, database is CAplus and MEDLINE.

A series of novel 2,4,5-trisubstituted 1,3-thiazole derivatives containing hydrazide-hydrazine and carboxamide moieties including 46 compounds T were synthesized, and evaluated for their antitumor activity in vitro against a panel of five human cancer cell lines. Eighteen title compounds T displayed higher inhibitory activity than that of 5-Fu against MCF-7, HepG2, BGC-823, Hela, and A549 cell lines. Especially, I, II, and III exhibit best cytotoxic activities with IC₅₀ values of 2.21 μg/mL, 1.67 μg/mL, and 1.11 μg/mL, against MCF-7, BCG-823, and HepG2 cell lines, resp. These results suggested that the combination of 1,3-thiazole, hydrazide-hydrazone, and carboxamide moieties was favorable to cytotoxicity activity. Furthermore, the flow cytometry anal. revealed that compounds I and III could induce apoptosis in HepG2 cells, and it was confirmed III led the induction of cell apoptosis by S cell-cycle arrest.

Bioorganic & Medicinal Chemistry 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, SDS of cas: 2447-79-2.

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

Zhang, Yue published the artcileAnderson-type polyoxometalate-based complexes constructed from a new ′V′-like bis-pyridine-bis-amide ligand for selective adsorption of organic dyes and detection of Cr(VI) and Fe(III) ions, Related Products of amides-buliding-blocks, the publication is Inorganic Chemistry Frontiers (2021), 8(20), 4458-4466, database is CAplus.

By introducing a new ′V′-like bis-pyridine-bis-amide ligand 4,4′-bis(4-pyridinecarboxamide)phenylmethane (L) into the reaction system based on Anderson-type polyoxometalates [XMo₆(OH)₆O₁₈]^3- (X = Al or Cr), four metal-organic complexes (MOCs) 1-4, [Zn(HL)(H₂O)₂(XMo₆(OH)₆O₁₈)].5H₂O (1: X = Al; 2: X = Cr), [Co(HL)(H₂O)₂(XMo₆(OH)₆O₁₈)]·5H₂O (3: X = Al; 4: X = Cr), have been prepared under solvothermal conditions, which have been characterized by single crystal X-ray diffraction, IR spectra, and PXRD. All structures of 1-4 involved a 2D layer that originated from XMo₆ polyoxoanions and metal ions, on both sides of which the L ligands were hanged. Complexes 1-4 showed not only outstanding selective adsorption capacities for organic dyes crystal violet, methylene blue and neutral red, but also electrochem. sensing behaviors toward Cr(VI) ions and Fe(III) ions with well-pleasing limits of detection of 0.606 nM (6.24 × 10-5 ppm) and 0.0192 μM (1.08 × 10-3 ppm), suggesting their potential application as multifunctional materials.

Inorganic Chemistry Frontiers 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 C8H11BO2, Related Products of amides-buliding-blocks.

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

Ma, Liang published the artcileSynthesis, Activity, and Docking Study of Novel Phenylthiazole-Carboxamido Acid Derivatives as FFA2 Agonists, Quality Control of 2447-79-2, the publication is Chemical Biology & Drug Design (2016), 88(1), 26-37, database is CAplus and MEDLINE.

Free fatty acid receptor 2 (FFA2), also known as GPR43, is activated by short-chain fatty acids (SCFAs) that are mainly produced by the gut microbiota through the fermentation of undigested carbohydrates and dietary fibers. FFA2 currently appears to be a potential target in the management of obesity, diabetes, inflammatory diseases, and cancer. In the study, a series of novel phenylthiazole-carboxamido acid derivatives has been synthesized and evaluated as potential orthosteric FFA2 ligands for the study of structure-activity relationships. Compound 6e was found to exhibit the twofold potent agonistic activity in the stable hFFA2-transfected CHO-K1 cells (EC₅₀ = 23.1 μm) as that of pos. control propionate (EC₅₀ = 43.3 μm). We also reported the results of mutagenesis studies based on the crystal structure of hFFA1 bound to TAK-875 at 2.3 Å resolution to identify important residues for orthosteric agonist 6e inducing FFA2 activation.

Chemical Biology & Drug Design 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, Quality Control of 2447-79-2.

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

Wei, Jing published the artcile3D-Pharmacophore Models for Selective A_2A and A_2B Adenosine Receptor Antagonists, Product Details of C27H29N5O5, the publication is Journal of Chemical Information and Modeling (2007), 47(2), 613-625, database is CAplus and MEDLINE.

Three-dimensional pharmacophore models were generated for A_2A and A_2B adenosine receptors (ARs) based on highly selective A_2A and A_2B antagonists using the Catalyst program. The best pharmacophore model for selective A_2A antagonists (Hypo-A_2A) was obtained through a careful validation process. Four features contained in Hypo-A_2A (one ring aromatic feature (R), one pos. ionizable feature (P), one hydrogen bond acceptor lipid feature (L), and one hydrophobic feature (H)) seem to be essential for antagonists in terms of binding activity and A_2A AR selectivity. The best pharmacophore model for selective A_2B antagonists (Hypo-A_2B) was elaborated by modifying the Catalyst common features (HipHop) hypotheses generated from the selective A_2B antagonists training set. Hypo-A_2B also consists of four features: one ring aromatic feature (R), one hydrophobic aliphatic feature (Z), and two hydrogen bond acceptor lipid features (L). All features play an important role in A_2B AR binding affinity and are essential for A_2B selectivity. Both A_2A and A_2B pharmacophore models have been validated toward a wide set of test mols. containing structurally diverse selective antagonists of all AR subtypes. They are capable of identifying correspondingly high potent antagonists and differentiating antagonists between subtypes. The results of our study will act as a valuable tool for retrieving structurally diverse compounds with desired biol. activities and designing novel selective adenosine receptor ligands.

Journal of Chemical Information and Modeling 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 C12H9N3O4, Product Details of C27H29N5O5.

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

Zhang, Lijun published the artcileCannizzaro-Type Disproportionation of Aromatic Aldehydes to Amides and Alcohols by Using Either a Stoichiometric Amount or a Catalytic Amount of Lanthanide Compounds, Recommanded Product: 2,4-Dichlorobenzamide, the publication is Journal of Organic Chemistry (2006), 71(8), 3149-3153, database is CAplus and MEDLINE.

Aromatic aldehydes can be directly converted to the corresponding amides and alcs. in good to excellent yields by treatment with LiN(SiMe₃)₂ in the presence of catalytic lanthanide chlorides LnCl₃ or with a stoichiometric amount of lanthanide amides [(Me₃Si)₂N]₃Ln(μ-Cl)Li(THF)₃ at ambient temperature. The effects of solvents, substituents on the Ph ring, and lanthanide metals on the reaction have been examined The mechanism of the disproportionation reaction was proposed based on the exptl. results.

Journal of Organic Chemistry 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 C5H10O2S, Recommanded Product: 2,4-Dichlorobenzamide.

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

Zheng, Chunxiong published the artcileIn Situ Modification of the Tumor Cell Surface with Immunomodulating Nanoparticles for Effective Suppression of Tumor Growth in Mice, COA of Formula: C10H12BNO5, the publication is Advanced Materials (Weinheim, Germany) (2019), 31(32), n/a, database is CAplus and MEDLINE.

Current cancer immunotherapies including chimeric antigen receptor (CAR)-based therapies and checkpoint immune inhibitors have demonstrated significant clin. success, but always suffer from immunotoxicity and autoimmune disease. Recently, nanomaterial-based immunotherapies are developed to precisely control in vivo immune activation in tumor tissues for reducing immune-related adverse events. However, little consideration has been put on the spatial modulation of interactions between immune cells and cancer cells to optimize the efficacy of cancer immunotherapies. Herein, a rational design of immunomodulating nanoparticles is demonstrated that can in situ modify the tumor cell surface with natural killer cell (NK cell)-activating signals to achieve in situ activation of tumor-infiltrating NK cells, as well as direction of their antitumor immunity toward tumor cells. Using these immunomodulating nanoparticles, the remarkable inhibition of tumor growth is observed in mice without noticeable side effects. This study provides an accurate immunomodulation strategy that achieves safe and effective antitumor immunity through in situ NK cell activation in tumors. Further development by constructing interactions with various immune cells can potentially make this nanotechnol. become a general platform for the design of advanced immunotherapies for cancer treatments.

Advanced Materials (Weinheim, Germany) published new progress about 2024542-05-8. 2024542-05-8 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Boronic Acids, name is 3-(4-Boronobenzamido)propanoic acid, and the molecular formula is C7H3Cl2F3O2S, COA of Formula: C10H12BNO5.

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

Li, Ling published the artcileActivation of p53 by SIRT1 Inhibition Enhances Elimination of CML Leukemia Stem Cells in Combination with Imatinib, Related Products of amides-buliding-blocks, the publication is Cancer Cell (2012), 21(2), 266-281, database is CAplus and MEDLINE.

BCR-ABL tyrosine kinase inhibitors (TKI) fail to eliminate quiescent leukemia stem cells (LSC) in chronic myelogenous leukemia (CML). Thus, strategies targeting LSC are required to achieve cure. We show that the NAD⁺-dependent deacetylase SIRT1 is overexpressed in human CML LSC. Pharmacol. inhibition of SIRT1 or SIRT1 knockdown increased apoptosis in LSC of chronic phase and blast crisis CML and reduced their growth in vitro and in vivo. SIRT1 effects were enhanced in combination with the BCR-ABL TKI imatinib. SIRT1 inhibition increased p53 acetylation and transcriptional activity in CML progenitors, and the inhibitory effects of SIRT1 targeting on CML cells depended on p53 expression and acetylation. Activation of p53 via SIRT1 inhibition represents a potential approach to target CML LSC.

Cancer Cell 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, Related Products of amides-buliding-blocks.

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

Ge, Yongmei published the artcileA ZIF-8-based multifunctional intelligent drug release system for chronic osteomyelitis, Formula: C17H14F3N3O2S, the publication is Colloids and Surfaces, B: Biointerfaces (2022), 112354, database is CAplus and MEDLINE.

Chronic osteomyelitis (COM) is an inflammatory bone disease caused by bacterial infection. Conventional treatment with antibiotics is prone to resistance and other side effects, and it is ineffective against inflammation caused by infection and bone loss. To treat COM comprehensively, based on the acidic microenvironment of osteomyelitis, we used ZIF-8 and celecoxib to construct a multifunctional intelligent drug release system with pH response effect, named CEL@ZIF-8. Material characterization revealed that celecoxib is successfully loaded into ZIF-8. Ion release and drug release experiments indicated that CEL@ZIF-8 can respond well to the pH and intelligently control the release of ions and drugs. Antibacterial assays manifested that CEL@ZIF-8 is able to inhibit the growth of bacteria significantly. In vitro cell experiments demonstrated that CEL@ZIF-8 can significantly up-regulate the expression of osteogenesis-related cytokines and down-regulate the levels of inflammatory factors. Studies verify that the novel drug release system possesses multiple functions: antibacterial, osteogenesis, anti-inflammatory and intelligent release, suggesting a tremendous clin. promise for the treatment of COM.

Colloids and Surfaces, B: Biointerfaces 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, Formula: C17H14F3N3O2S.

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