Author: tianli

Kadota, Ayano; Moriguchi, Misato; Watanabe, Tadashi; Sekine, Yuichi; Nakamura, Shigeo; Yasuno, Takumi; Ohe, Tomoyuki; Mashino, Tadahiko; Fujimuro, Masahiro published the artcile< A pyridinium-type fullerene derivative suppresses primary effusion lymphoma cell viability via the downregulation of the Wnt signaling pathway through the destabilization of β-catenin>, Product Details of C11H8N2O3S2, the main research area is Wnt beta catenin pyridinium fullerene suppression primary effusion lymphoma; Kaposi’s sarcoma‑associated herpesvirus; Wnt signaling; fullerene; primary effusion lymphoma; pyridinium fullerene; β‑catenin.

Primary effusion lymphoma (PEL) is defined as a rare subtype of non-Hodgkin′s B cell lymphoma, which is caused by Kaposi′s sarcoma-associated herpesvirus (KSHV) in immunosuppressed patients. PEL is an aggressive type of lymphoma and is frequently resistant to conventional chemo- therapeutics. Therefore, the discovery of novel drug candidates for the treatment of PEL is of utmost importance. In order to discover potential novel anti-tumor compounds against PEL, the authors previously developed a pyrrolidinium-type fullerene derivative, 1,1,1′,1′-tetramethyl [60]fullerenodi- pyrrolidinium diiodide (derivative #1), which induced the apoptosis of PEL cells via caspase-9 activation. In the present study, the growth inhibitory effects of pyrrolidinium-type (derivatives #1 and #2), pyridinium-type (derivatives #3 and #5 to #9) and anilinium-type fullerene derivatives (derivative #4) against PEL cells were evaluated. This anal. revealed a pyridinium-type derivative (derivative #5; 3-5′-(ethoxycarbonyl)-1′,5′-dihydro-2′H-[5,6]fullereno-C60-Ih-[1,9-c] pyrrol-2′-yl-1-methylpyridinium iodide), which exhibited antitumor activity against PEL cells via the downregulation of Wnt/β-catenin signaling. Derivative #5 suppressed the viability of KSHV-infected PEL cells compared with KSHV-uninfected B-lymphoma cells. Furthermore, derivative #5 induced the destabilization of β-catenin and suppressed β-catenin-TCF4 transcriptional activity in PEL cells. It is known that the constitutive activation of Wnt/β-catenin signaling is essential for the growth of KSHV-infected cells. The Wnt/β-catenin activation in KSHV-infected cells is mediated by KSHV latency-associated nuclear antigen (LANA). The data demonstrated that derivative #5 increased β-catenin phosphorylation, which resulted in β-catenin polyubiquitination and subsequent degradation Thus, derivative #5 overcame LANA-mediated β-catenin stabilization. Furthermore, the administration of derivative #5 suppressed the development of PEL cells in the ascites of SCID mice with tumor xenografts derived from PEL cells. On the whole, these findings provide evidence that the pyridinium-type fullerene derivative #5 exhibits antitumor activity against PEL cells in vitro and in vivo. Thus, derivative #5 may be utilized as a novel therapeutic agent for the treatment of PEL.

Oncology Reports published new progress about Adenomatous polyposis coli proteins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Product Details of C11H8N2O3S2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

He, Bai; Velaparthi, Subash; Pieffet, Gilles; Pennington, Chris; Mahesh, Aruna; Holzle, Denise L.; Brunsteiner, Michael; van Breemen, Richard; Blond, Sylvie Y.; Petukhov, Pavel A. published the artcile< Binding Ensemble Profiling with Photoaffinity Labeling (BEProFL) Approach: Mapping the Binding Poses of HDAC8 Inhibitors>, Synthetic Route of 57493-24-0, the main research area is histone deacetylase HDAC8 photoaffinity labeling BEProFL.

A binding ensemble profiling with (f)photoaffinity labeling (BEProFL) approach that utilizes photolabeling of HDAC8 with a probe containing a UV-activated aromatic azide, mapping of the covalent modifications by liquid chromatog.-tandem mass spectrometry, and a computational method to characterize the multiple binding poses of the probe is described. By use of the BEProFL approach, two distinct binding poses of the HDAC8 probe were identified. The data also suggest that an “”upside-down”” pose with the surface binding group of the probe bound in an alternative pocket near the catalytic site may contribute to the binding.

Journal of Medicinal Chemistry published new progress about Enzyme functional sites. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Synthetic Route of 57493-24-0.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Choi, Sunju; Matta, Hittu; Gopalakrishnan, Ramakrishnan; Natarajan, Venkatesh; Gong, Songjie; Jeronimo, Alberto; Kuo, Wei-Ying; Bravo, Bryant; Chaudhary, Preet M. published the artcile< A novel thermostable beetle luciferase based cytotoxicity assay>, SDS of cas: 2591-17-5, the main research area is luciferase thermostability isolation beetle anticancer agent cytotoxicity.

Cytotoxicity assays are essential for the testing and development of novel immunotherapies for the treatment of cancer. We recently described a novel cytotoxicity assay, termed the Matador assay, which was based on marine luciferases and their engineered derivatives In this study, we describe the development of a new cytotoxicity assay termed ‘Matador-Glo assay’ which takes advantage of a thermostable variant of Click Beetle Luciferase (Luc146-1H2). Matador-Glo assay utilizes Luc146-1H2 and D-luciferin as the luciferase-substrate pair for luminescence detection. The assay involves ectopic over-expression of Luc146-1H2 in the cytosol of target cells of interest. Upon damage to the membrane integrity, the Luc146-1H2 is either released from the dead and dying cells or its activity is preferentially measured in dead and dying cells. We demonstrate that this assay is simple, fast, specific, sensitive, cost-efficient, and not labor-intensive. We further demonstrate that the Matador-Glo assay can be combined with the marine luciferase-based Matador assay to develop a dual luciferase assay for cell death detection. Finally, we demonstrate that the Luc146-1H2 expressing target cells can also be used for in vivo bioluminescence imaging applications.

Scientific Reports published new progress about Antitumor agents. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, SDS of cas: 2591-17-5.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Farmer, Luc J.; Bemis, Guy; Britt, Shawn D.; Cochran, John; Connors, Martin; Harrington, Edmund M.; Hoock, Thomas; Markland, William; Nanthakumar, Suganthini; Taslimi, Paul; Ter Haar, Ernst; Wang, Jian; Zhaveri, Darshana; Salituro, Francesco G. published the artcile< Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK)>, Electric Literature of 20582-55-2, the main research area is pyrimidine phenylamino thiazolyl derivative preparation tyrosine kinase inhibition SAR; phenylamino pyrimidine thiazole derivative preparation mast cell degranulation inhibition.

A series of SYK inhibitors based on the phenylamino pyrimidine thiazole lead, I, were prepared and evaluated for biol. activity. Lead optimization provided compounds with nanomolar Ki’s against SYK and potent inhibition in mast cell degranulation assays.

Bioorganic & Medicinal Chemistry Letters published new progress about Animal gene, c-src Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Electric Literature of 20582-55-2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Bi, Huihua; Zhou, Yu; Jiang, Wei; Liu, Jie published the artcile< Electrophotocatalytic C-H Hydroxyalkylation of Heteroaromatics with Aldehydes>, Synthetic Route of 20582-55-2, the main research area is heteroarene electrochem photochem Minisci hydroxyalkylation aldehyde; alc heteroaryl preparation.

A radical hydroxyalkylation of N-heteroaromatics with aldehydes is reported. The constructive merging of photochem. and electrochem. is the key for the success of this atom-economical Minisci method. This protocol highlights the utility of electrophotocatalysis to promote a practical and general synthesis of secondary alcs. in good yields from readily available N-heteroaromatics and aldehydes under mild reaction conditions.

Advanced Synthesis & Catalysis published new progress about Aldehydes Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Synthetic Route of 20582-55-2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Zielonka, Jacek; Podsiadly, Radoslaw; Zielonka, Monika; Hardy, Micael; Kalyanaraman, Balaraman published the artcile< On the use of peroxy-caged luciferin (PCL-1) probe for bioluminescent detection of inflammatory oxidants in vitro and in vivo - Identification of reaction intermediates and oxidant-specific minor products>, HPLC of Formula: 115144-35-9, the main research area is inflammatory oxidant bioluminescence probe peroxy caged luciferin; Bioluminescence; Boronate probes; Luciferin; Spin traps.

Peroxy-caged luciferin (PCL-1)(I) probe was first used to image hydrogen peroxide in living systems (Van de Bittner et al., 2010 [9]). Recently this probe was shown to react with peroxynitrite more potently than with hydrogen peroxide (Sieracki et al., 2013 [11]) and was suggested to be a more suitable probe for detecting peroxynitrite under in vivo conditions. In this work, we investigated in detail the products formed from the reaction between PCL-1 and hydrogen peroxide, hypochlorite, and peroxynitrite. HPLC anal. showed that hydrogen peroxide reacts slowly with PCL-1, forming luciferin as the only product. Hypochlorite reaction with PCL-1 yielded significantly less luciferin, as hypochlorite oxidized luciferin to form a chlorinated luciferin. Reaction between PCL-1 and peroxynitrite consists of a major and minor pathway. The major pathway results in luciferin and the minor pathway produces a radical-mediated nitrated luciferin. Radical intermediate was characterized by spin trapping. We conclude that monitoring of chlorinated and nitrated products in addition to bioluminescence in vivo will help identify the nature of oxidant responsible for bioluminescence derived from PCL-1.

Free Radical Biology & Medicine published new progress about Bioluminescence. 115144-35-9 belongs to class thiazole, and the molecular formula is C11H7KN2O3S2, HPLC of Formula: 115144-35-9.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Nath, J. P.; Dash, Manjula; Satrusallya, S. C.; Mahapatra, G. N. published the artcile< Synthesis of some 7-substituted 8-hydroxyquinoline derivatives of thiazoles and oxazoles as potential pesticides>, Safety of 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is hydroxyquinoline fungicide bactericide pesticide preparation; aminomethylhydroxyquinoline thiazolyl oxazolyl; Mannich hydroxyquinoline.

Mannich reaction of 8-hydroxyquinoline with PhCHO and I (R = H, Cl, Br; R1 = Ph, 4-ClC6H4, 4-BrC6H4, 4-HOC6H4, 4-MeO(C6H4, 3-O2NC6H4, 4-O2NC6H4, 4-MeC6H4, α-,β-naphthyl; X = O, S) gave the title compounds (II). II showed bactericidal and fungicidal activity.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about Fungicides. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Safety of 2-Amino-4-(3-nitrophenyl)thiazole.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Patel, Snahel; Harris, Seth F.; Gibbons, Paul; Deshmukh, Gauri; Gustafson, Amy; Kellar, Terry; Lin, Han; Liu, Xingrong; Liu, Yanzhou; Liu, Yichin; Ma, Changyou; Scearce-Levie, Kimberly; Ghosh, Arundhati Sengupta; Shin, Young G.; Solanoy, Hilda; Wang, Jian; Wang, Bei; Yin, Jianping; Siu, Michael; Lewcock, Joseph W. published the artcile< Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12)>, Application In Synthesis of 324579-90-0, the main research area is preparation pyrazolylpyridinamine leucine zipper kinase inhibitor.

Recent data suggest that inhibition of dual leucine zipper kinase (DLK, MAP3K12) has therapeutic potential for treatment of a number of indications ranging from acute neuronal injury to chronic neurodegenerative disease. Thus, high demand exists for selective small mol. DLK inhibitors with favorable drug-like properties and good CNS penetration. Herein the authors describe a shape-based scaffold hopping approach to convert pyrimidine 1 to a pyrazole core with improved physicochem. properties. The authors also present the first crystal structures of DLK. By utilizing a combination of property and structure-based design, the authors identified inhibitor I, a potent, selective, and brain-penetrant inhibitor of DLK with activity in an in vivo nerve injury model.

Journal of Medicinal Chemistry published new progress about Blood-brain barrier. 324579-90-0 belongs to class thiazole, and the molecular formula is C6H8N2S, Application In Synthesis of 324579-90-0.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Zhu, Yan-Ping; Yuan, Jing-Jing; Zhao, Qin; Lian, Mi; Gao, Qing-He; Liu, Mei-Cai; Yang, Yan; Wu, An-Xin published the artcile< I2/CuO-catalyzed tandem cyclization strategy for one-pot synthesis of substituted 2-aminothiazole from easily available aromatic ketones/α,β-unsaturated ketones and thiourea>, Category: thiazole, the main research area is aminothiazole preparation thiourea aromatic ketone butenone cyclization.

A concise and efficient one-pot process from easily available Me ketones or unsaturated Me ketones and thiourea was developed for the synthesis of 2-aminothiazoles with I2/CuO as catalyst. The method gave the E-isomers of 4-ethenyl-2-aminothiazoles. All these target mols. were characterized by NMR, HRMS and IR spectra.

Tetrahedron published new progress about 1,3-Dicarbonyl compounds Role: RCT (Reactant), RACT (Reactant or Reagent). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Category: thiazole.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Kitir, Betul; Baldry, Mara; Ingmer, Hanne; Olsen, Christian A. published the artcile< Total synthesis and structural validation of cyclodepsipeptides solonamide A and B>, Name: (S)-4-Benzylthiazolidine-2-thione, the main research area is cyclodepsipeptide solonamide A B total enantioselective synthesis antimicrobial; macrocycle virulence gene expression Staphylococcus aureus inhibitor cyclodepsipeptide; hydroxy acid stereoselective aldol reaction esterification acylation macrolactamization.

Microorganisms are an attractive source of new natural products with antimicrobial properties, and the marine environment constitutes a prolific resource of bioactive microorganisms. During a global research expedition (Galathea III), two depsipeptides, solonamide A and solonamide B, were isolated from the marine bacterium Photobacterium halotolerance and were found to inhibit virulence gene expression in the serious human pathogen, Staphylococcus aureus. They act by interfering with the agr quorum sensing system and show resemblance to the endogenous S. aureus quorum sensing peptide, autoinducing peptide I (AIP-I). To enable more comprehensive studies, we embarked on the chem. synthesis of solonamides A and B. The key synthetic steps were formation of the (R)-β-hydroxy-fatty-acids by stereoselective aldol reactions and a cyclative macrolactamization, which proceeded under highly dilute conditions. Thus, the first total syntheses of the solonamides corroborated the originally assigned structures, and by changing the stereochem. of the auxiliary in the aldol steps we gained access to the natural products as well as their β3-epimers.

Tetrahedron published new progress about Acylation. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Name: (S)-4-Benzylthiazolidine-2-thione.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica