Month: December 2022

Sun, Jiangtao published the artcileTargeting histone deacetylase SIRT1 selectively eradicates EGFR TKI-resistant cancer stem cells via regulation of mitochondrial oxidative phosphorylation in lung adenocarcinoma, SDS of cas: 1011557-82-6, the publication is Neoplasia (New York, NY, United States) (2020), 22(1), 33-46, database is CAplus and MEDLINE.

Lung adenocarcinoma (LAD) is a human malignancy successfully treated with the tyrosine kinase inhibitor (TKI) gefitinib; however, the enrichment of therapy resistant cancer stem cells (CSCs) in such patients is assumed to be a source of treatment failure. Evaluation of LAD cell populations treated with the TKI inhibitor gefitinib identified unique aspects of a subpopulation of tumor cells exhibiting stem-like properties and mitochondria-specific metabolic features along with their reliance on sirtuin 1 (SIRT1) for survival advantage. Accordingly, loss of the phenotype present in resistant CSC clones either by targeting the energy metabolism with tigecycline or tenovin-6 inhibited their dependency on mtOXPHOS and sensitized them for a more pronounced and long-lasting TKI therapeutic effect. The results specifically demonstrated that combined therapy with TV-6 and gefitinib resulted in tumor regression in xenograft mouse models, whereas administration of a single agent showed no such efficacy. Importantly, combined treatment with TV-6 also decreased the ED of gefitinib necessary for treatment response. Clin. anal. demonstrated that high-profile SIRT1 and mtOXPHOS proteins were associated with recurrence and poor prognosis in LAD patients. These observations support the CSC hypothesis for cancer relapse and advocate use of mitochondria-targeting inhibitors as part of combinatorial therapy in a variety of clin. settings, as well as for reducing TKI dosage in LAD patients.

Neoplasia (New York, NY, United States) 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 C5H9IO2, SDS of cas: 1011557-82-6.

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

Chen, Enjiang published the artcilemiR-26b enhances the sensitivity of hepatocellular carcinoma to Doxorubicin via USP9X-dependent degradation of p53 and regulation of autophagy, SDS of cas: 380315-80-0, the publication is International Journal of Biological Sciences (2021), 17(3), 781-795, database is CAplus and MEDLINE.

Multi-drug resistance is a major challenge to hepatocellular carcinoma (HCC) treatment, and the over-expression or deletion of microRNA (miRNA) expression is closely related to the drug-resistant properties of various cell lines. However, the underlying mol. mechanisms remain unclear. CCK-8, EdU, flow cytometry, and transmission electron microscopy were performed to determine cell viability, proliferation, apoptosis, autophagic flow, and nanoparticle characterization, resp. In this study, the results showed that the expression of miR-26b was downregulated following doxorubicin treatment in human HCC tissues. An miR-26b mimic enhanced HCC cell doxorubicin sensitivity, except in the absence of p53 in Hep3B cells. Delivery of the proteasome inhibitor, MG132, reversed the inhibitory effect of miR-26b on the level of p53 following doxorubicin treatment. Tenovin-1 (an MDM2 inhibitor) protected p53 from ubiquitination-mediated degradation only in HepG2 cells with wild type p53. Tenovin-1 pretreatment enhanced HCC cell resistance to doxorubicin when transfected with an miR-26b mimic. Moreover, the miR-26b mimic inhibited doxorubicin-induced autophagy and the autophagy inducer, rapamycin, eliminated the differences in the drug sensitivity effect of miR-26b. In vivo, treatment with sp94dr/miR-26b mimic nanoparticles plus doxorubicin inhibited tumor growth. Our current data indicate that miR-26b enhances HCC cell sensitivity to doxorubicin through diminishing USP9X-mediated p53 de-ubiquitination caused by DNA damaging drugs and autophagy regulation. This miRNA-mediated pathway that modulates HCC will help develop novel therapeutic strategies.

International Journal of Biological Sciences 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 C20H23N3O2S, SDS of cas: 380315-80-0.

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

Yan, Jing published the artcileEffect of Yiqi Huayu Pinggan Zishen Formula Combined with Valsartan in the Treatment of Hypertension and Its Effect on MMP-9, Ang II, and MCP-1., Recommanded Product: (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, the publication is Computational and mathematical methods in medicine (2022), 7982023, database is MEDLINE.

Objective: To explore the effect of Yiqi Huayu Pinggan Zishen recipe combined with valsartan in the treatment of hypertension and its effect on MMP-9, Ang II, and MCP-1. Methods: About 100 patients with hypertension treated in our hospital from March 2020 to April 2021 were enrolled. All patients were arbitrarily assigned to the control group and the study group. The former group was cured with valsartan, and the latter group was cured with Yiqi Huayu Pinggan Zishen recipe combined with valsartan. The curative effect, blood pressure level, renal function index, serum matrix metalloproteinase-9 (MMP-9), monocyte chemoattractant protein-1 (MCP-1), angiotensin II (Ang II) level, traditional Chinese medicine (TCM) syndrome score, and the incidence of adverse reactions were compared. Results: First of all, we compared the curative effects; the study group exhibited remarkably effective in 44 cases and effective in 6 cases, and the effective rate was 100.00%, while in the control group, 24 cases were markedly effective, 16 cases were effective, and 5 cases were ineffective; the effective rate was 90.00%. The curative effect in the study group was higher (P < 0.05). Secondly, we compared the blood pressure level. Before treatment, there was no remarkable difference (P > 0.05). After treatment, the blood pressure of the two groups decreased. The systolic blood pressure and diastolic blood pressure of the study group were lower (P < 0.05). In terms of renal function indexes, the levels of blood urine nitrogen (BUN), Cr, and β 2-MG in the study group were lower, while the level of eGFR in the study group was higher (P < 0.05). The serum levels of MMP-9, MCP-1, and Ang II decreased. Of note, the levels of serum MMP-9, MCP-1, and Ang II in the study group were lower (P < 0.05). After treatment, the TCM syndrome scores decreased, and the study group was lower (P < 0.05). Finally, we compared the incidence of adverse reactions. The incidence of adverse reactions in the study group was lower (P < 0.05). Conclusion: Yiqi Huayu Pinggan Zishen recipe combined with valsartan in the treatment of hypertension can remarkably reduce the clinical symptoms, enhance the renal function, strengthen the therapeutic effect, promote the ability of independent movement, and reduce the levels of serum MMP-9, MCP-1, and Ang II with high safety, which has the value of clinical application.

Computational and mathematical methods in medicine 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 C10H6F17N, Recommanded Product: (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid.

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

Zhang, Tian-Yi published the artcileNew ursolic acid derivatives bearing 1,2,3-triazole moieties: design, synthesis and anti-inflammatory activity in vitro and in vivo, Formula: C17H14F3N3O2S, the publication is Molecular Diversity (2022), 26(2), 1129-1139, database is CAplus and MEDLINE.

In order to discover novel anti-inflammatory agents, three series of compounds obtained by appending 1,2,3-triazole moieties on ursolic acid I [n = 3; R¹ = H, 2-F, 4-Me, 3,4-(CH₃)₂], II [R² = H, 3-OMe, 2,4-(CH₃)₂, 3-CF₃, 2,4-Cl₂; X = O, NH], III (R³ = Ph, 2,3-dimethoxyphenyl, furan-2-yl, etc.) were designed and synthesized. All compounds have been screened for their anti-inflammatory activity by using an ear edema model. The potent anti-inflammatory compound was subjected to in vitro cyclooxygenase COX-1/COX-2 inhibition assays. In general, the derivatives were found to be potent anti-inflammatory activity. Especially, the compound I (n = 3; R³ = 2,3-dimethoxyphenyl) (IV) exhibited the strongest activity of all of the compounds prepared, with 82.81% inhibition after i.p. administration, which was better than celecoxib as a pos. control. Mol. docking results unclose the rationale for the interaction of the compound IV with COX-2 enzyme. Further studies revealed that compound IV exhibited effective COX-2 inhibitory activity, with half-maximal inhibitor concentration (IC₅₀) value of 1.16μM and selectivity index (SI = 64.66) value close to that of celecoxib (IC₅₀ = 0.93μM, SI = 65.47). Taken together, these results could suggest a promising chemotype for development of new COX-2-targeting anti-inflammatory agent.

Molecular Diversity 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 C10H11NO4, Formula: C17H14F3N3O2S.

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

Wang, Yueqi published the artcileA reactive oxygen species-responsive dendrimer with low cytotoxicity for efficient and targeted gene delivery, HPLC of Formula: 1869-45-0, the publication is Chinese Chemical Letters (2020), 31(1), 275-280, database is CAplus.

Nonviral vectors have been attracting more attention for several advantages in gene delivery and the development of nonviral gene carriers with high delivery efficiency and low cytotoxicity has long been a key project. Starburst polyamidoamine dendrimers are a class of synthetic polymers with unique structural and phys. characteristics. However, when they are used as gene carrier, the gene transfection efficiency is not satisfactory. Herein, a novel thioketal-core polyamidoamine dendrimer (i.e., ROS-PAMAM) was synthesized and characterized. Compared to ethylenediamine-core dendrimers or widely used cationic polymers of polyetherimide, ROS-PAMAM showed lower cytotoxicity. Moreover, ROS-PAMAM demonstrated reactive oxygen species responsive characteristics, which can facilitate the release of siRNA in the tumor microenvironment. In vitro gene transfection experiments based on A549 cells confirmed that siRNA/ROS-PAMAM exhibits high gene transfection efficiency. It is concluded that ROS-PAMAM shows great potential as a generalizable vehicle for gene therapy applications.

Chinese Chemical Letters 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 C19H21N3O3S, HPLC of Formula: 1869-45-0.

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

Yuan, Zhefan published the artcileZwitterionic Peptide Cloak Mimics Protein Surfaces for Protein Protection, Application of H-Lys(Boc)-OH, the publication is Angewandte Chemie, International Edition (2020), 59(50), 22378-22381, database is CAplus and MEDLINE.

Inspired by the amino acid composition of natural protein surfaces, we developed a zwitterionic cloak containing multi-layers of short alternating glutamic acid and lysine (EK) peptides as a facile, highly effective and low-immunogenicity approach for the protection and delivery of biotherapeutics. Each EK layer grafted to proteins provides multiple times of new lysine reaction sites for the growth of subsequent EK layers. This unique design allows EK peptides to achieve high coating d. on proteins, overcoming the limitation of traditional conjugation strategies that rely on the number of innate lysine groups. A triple-layer EK cloak manifests to successfully eliminate the specific and non-specific interactions of protected asparaginase with biol. media while prolong the drug circulation time and significantly mitigate its immunogenicity in vivo, suggesting an EK peptide cloak as a promising approach to improve the safety and efficacy of biotherapeutics.

Angewandte Chemie, International Edition 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 Al2H32O28S3, Application of H-Lys(Boc)-OH.

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

Zhou, Jun published the artcileRhodium(III)-catalyzed oxidative olefination of picolinamides: Convenient synthesis of 3-alkenylpicolinamides, Category: amides-buliding-blocks, the publication is Advanced Synthesis & Catalysis (2014), 356(5), 1038-1046, database is CAplus.

A rhodium(III)-catalyzed selective olefination of picolinamide derivatives has been developed. The reaction shows high regioselectivity, low catalyst loading (0.5 mol%), high yield, and good functional group tolerance, providing a convenient strategy for the synthesis of 3-alkenylpicolinamides.

Advanced Synthesis & Catalysis published new progress about 530-40-5. 530-40-5 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N,N-Diethylisonicotinamide, and the molecular formula is C28H41N7O4, Category: amides-buliding-blocks.

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

Han, Boyang published the artcileConstruction of cyclophane-braced peptide macrocycles via palladium-catalyzed picolinamide-directed intramolecular C(sp²)-H arylation, Category: amides-buliding-blocks, the publication is Organic Letters (2020), 22(17), 6879-6883, database is CAplus and MEDLINE.

A versatile method for the construction of C(sp²)-linked cyclophane peptide macrocycles via Pd-catalyzed picolinamide-directed intramol. arylation of aryl and alkenyl C-H bonds of amino acid side chains with aryl iodides is developed. This method provides simple and efficient access to a variety of cyclophane-braced structures from readily accessible linear peptide precursors.

Organic Letters 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

Seng, Florin published the artcile2-Aminocarbonyl-1-hydroxybenzimidazole 3-oxides, Application In Synthesis of 15029-36-4, the publication is Synthesis (1972), 606, database is CAplus.

The 1-hydroxybenzimidazole 3-oxides I (R = H, Cl, Me, OMe; R1 = H, Me, Et, Ph, cyclohexyl) were prepared in 32-92% yield by treating the corresponding benzofuroxans with NCCH2CONHR1 and aqueous NaOH to precipitate the Na salts of I. Acidification of the Na salts yielded free I.

Synthesis 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 C15H19BO2, Application In Synthesis of 15029-36-4.

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

Serezani, Carlos H. published the artcileLeukotriene B₄ amplifies NF-κB activation in mouse macrophages by reducing SOCS1 inhibition of MyD88 expression, COA of Formula: C12H23N3S, the publication is Journal of Clinical Investigation (2011), 121(2), 671-682, database is CAplus and MEDLINE.

Activation of NF-κB and 5-lipoxygenase-mediated (5-LO-mediated) biosynthesis of the lipid mediator leukotriene B₄ (LTB₄) are pivotal components of host defense and inflammatory responses. However, the role of LTB₄ in mediating innate immune responses elicited by specific TLR ligands and cytokines is unknown. Here we have shown that responses dependent on MyD88 (an adaptor protein that mediates signaling through all of the known TLRs, except TLR3, as well as IL-1β and IL-18) are reduced in mice lacking either 5-LO or the LTB₄ receptor BTL1, and that macrophages from these mice are impaired in MyD88-dependent activation of NF-κB. This macrophage defect was associated with lower basal and inducible expression of MyD88 and reflected impaired activation of STAT1 and overexpression of the STAT1 inhibitor SOCS1. Expression of MyD88 and responsiveness to the TLR4 ligand LPS were decreased by Stat1 siRNA silencing in WT macrophages and restored by Socs1 siRNA in 5-LO-deficient macrophages. These results uncover a pivotal role in macrophages for the GPCR BLT1 in regulating activation of NF-κB through Stat1-dependent expression of MyD88.

Journal of Clinical Investigation 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 C26H31N3O3, COA of Formula: C12H23N3S.

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