Tag: M.W:300-400

Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology. 120-78-5, Name is 2,2-Dithiobis(benzothiazole), molecular formula is , belongs to thiazoles compound. In a document, author is Takimoto, Tatsuya, Product Details of 120-78-5.

Simple Synthesis of a Heterocyclophane Exhibiting Anti-c-Met Activity by Acting as a Hatch Blocking Access to the Active Site**

A simple approach to the synthesis of heterocyclophane consisting of two 4,4′-bithiazoles has been developed in mild conditions. The heterocyclophane with two short chains was conveniently prepared by Hantzsch thiazoles synthesis using the reaction of 3-tert-butoxycarbonyl-3-azapentanethiocarboxamide with 1,4-dibromobutane-2,3-dione in methanol under reflux for only 15 min. Amino groups at the linkers of this heterocyclophane can be functionalized to give acylated and carbamate derivatives. Their properties as protein kinase inhibitors were investigated, and one of the heterocyclophanes exhibited specific anti-activity for c-mesenchymal epithelial transition factor (IC50=603 nm), among seven types of protein kinases investigated. The computational site identification by ligand competitive saturation method was used to determine why the one heterocyclophane exhibited strong anti-activity for c-mesenchymal epithelial transition factor.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 120-78-5, in my other articles. Product Details of 120-78-5.

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

Electric Literature of 76824-35-6, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 76824-35-6, Name is Famotidine, SMILES is N=C(NS(=O)(N)=O)CCSCC1=CSC(NC(N)=N)=N1, belongs to thiazoles compound. In a article, author is Ammar, Usama M., introduce new discover of the category.

Modification of imidazothiazole derivatives gives promising activity in B-Raf kinase enzyme inhibition; synthesis, in vitro studies and molecular docking

B-Raf mutation was identified as a key target in cancer treatment. Based on structural features of dabrafenib (potent FDA approved B-Raf inhibitor), the design of new NH2-based imidazothiazole derivatives was carried out affording new highly potent derivatives of imidazothiazole-based scaffold with amino substitution on the terminal phenyl ring as well as side chain with sulfonamide group and terminal substituted phenyl ring. In vitro enzyme assay was investigated against V600E B-Raf kinase. Compounds 10l, 10n and 10o showed higher inhibitory activities (IC50 = 1.20, 4.31 and 6.21 nM, respectively). In vitro cytotoxicity evaluation was assessed against NCI-60 cell lines. Most of tested derivatives showed cytotoxic activities against melanoma cell line. Compound 10k exhibited most potent activity (IC50 = 2.68 mu M). Molecular docking study revealed that the new designed derivatives preserved the same binding mode of dabrafenib with V600E B-Raf active site. It was investigated that the new modification in the synthesized derivatives (substituted with NH2) had a significant inhibitory activity towards V600E B-Raf. This core scaffold is considered a key compound for further structural and molecular optimization.

Electric Literature of 76824-35-6, One of the oldest and most widely used commercial enzyme inhibitors is aspirin, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 76824-35-6.

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

Electric Literature of 76824-35-6, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, 76824-35-6, Name is Famotidine, SMILES is N=C(NS(=O)(N)=O)CCSCC1=CSC(NC(N)=N)=N1, belongs to thiazoles compound. In a article, author is Lee, En Ting Tabitha, introduce new discover of the category.

Small molecule-PNA oligomer conjugates for rRNA A-site at neutral pH for FID assays

A triplex-forming PNA oligomer conjugated with a naphthyridine derivative (ATMND-C-2-NH2) showed high selectivity and strong binding for the bacterial rRNA A-site at pH 7.0 (K-d = 190 +/- 72 nM), which was accompanied by fluorogenic signaling that allowed the potential use of this conjugate probe in fluorescent indicator displacement assays.

Electric Literature of 76824-35-6, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 76824-35-6.

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

Electric Literature of 120-78-5, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 120-78-5, Name is 2,2-Dithiobis(benzothiazole), SMILES is C1(SSC2=NC3=CC=CC=C3S2)=NC4=CC=CC=C4S1, belongs to thiazoles compound. In a article, author is Cai, Xiaobing, introduce new discover of the category.

Thiostrepton and miR-216b synergistically promote osteosarcoma cell cytotoxicity and apoptosis by targeting FoxM1

Osteosarcoma is a common primary bone cancer that there are currently no effective treatment strategies for. Forkhead box M1 (FoxM1) is key in the development of osteosarcoma, and microRNA (miR)-216b serves an antitumor role by targeting FoxM1. Moreover, thiostrepton (TST), a natural thiazole antibiotic, induces antitumor effects and specifically targets FoxM1. Therefore, the present study investigated whether thiostrepton and miR-216b synergistically inhibited osteosarcoma cells by targeting FoxM1. The MTT assay, reverse transcription-quantitative PCR, a dual-luciferase reporter assay and flow cytometry were performed. Compared with the human osteoblast cell line hFOB1.19, miR-216b expression was significantly downregulated in the osteosarcoma cell lines U2OS, MG63 and Saos-2. By contrast, FoxM1 expression was significantly upregulated in osteosarcoma cell lines compared with the hFOB1.19 cell line. The results indicated that miR-216b targeted the 3 ‘-untranslated region of FoxM1. Moreover, the results suggested that miR-216b cooperated with TST to decrease cell cytotoxicity and increase cell apoptosis. In addition, miR-216b cooperated with TST to increase Bax expression and decrease Bcl-2 expression. In conclusion, the combination of TST and miR-216b synergistically promoted osteosarcoma cell cytotoxicity and apoptosis by targeting FoxM1. Therefore, the present study suggested that the combination of TST and miR-216b may serve as a promising therapeutic strategy for osteosarcoma.

Electric Literature of 120-78-5, The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 120-78-5 is helpful to your research.

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

In an article, author is Ali, Danish, once mentioned the application of 76824-35-6, Computed Properties of C8H15N7O2S3, Name is Famotidine, molecular formula is C8H15N7O2S3, molecular weight is 337.4454, MDL number is MFCD00079297, category is thiazoles. Now introduce a scientific discovery about this category.

Hydrogen Peroxide-Mediated Rapid Room Temperature Metal-Free C(sp(2))-H Thiocyanation of Amino Pyrazoles, Amino Uracils, and Enamines

A rapid metal- and additive-free room temperature method for C(sp(2))-H thiocyanation of aminopyrazoles, aminoisoxazole, aminoisothiazole, amino uracils, and aliphatic enamines has been developed in an aqueous medium using hydrogen peroxide as a benign oxidant and ammonium thiocyanate as a thiocyanating agent. On the other hand, the reaction of hydrogen peroxide and ammonium thiocyanate followed by one-pot addition of NaOH provides the corresponding disulfides in the case of amino azoles, and pyrimidine-fused 2-amino thiazoles were observed in the case of aminouracils. The salient features of this method are the use of an eco-friendly oxidant, reaction tunability to access different products, wide substrate scope, and good to very good yields.

If you are interested in 76824-35-6, you can contact me at any time and look forward to more communication. Computed Properties of C8H15N7O2S3.

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

In an article, author is Wang, Jun, once mentioned the application of 120-78-5, Name is 2,2-Dithiobis(benzothiazole), molecular formula is C14H8N2S4, molecular weight is 332.4867, MDL number is MFCD00022874, category is thiazoles. Now introduce a scientific discovery about this category, Quality Control of 2,2-Dithiobis(benzothiazole).

Novel eIF4E/eIF4G protein-protein interaction inhibitors DDH-1 exhibits anti-cancer activity in vivo and in vitro

(E)-2-(2-(2,3-dibromo-4,5-dimethoxybenzylidene)hydrazinyl)-4-(3,4-difluorophenyl) thiazole (DDH-1) is novel small molecule compound synthesized in our previous work. This study found that DDH-1 could inhibit the proliferation of various human lung cancer cells. Particularly, the IC50 for A549 cells was 8.59 AM. Interestingly, we found that DDH-1 inhibits eIF4E/eIF4G interaction. The flow cytometry (FAGS) results have indicated that DDH-1 may induce G0/G1 cycle arrest by inhibiting the expression of Cyclin D1 and CDK4. DDH-1 may also cause apoptosis through the caspase-dependent pathway. Study of these mechanisms has shown that DDH-1 may prompt reactive oxygen species (ROS) generation, decrease the mitochondrial membrane potential (MMP), and stimulate DNA double-strand breaks (DSBs) in A549 cells. Study of the signal pathway has indicated that DDH-1 could activate JNK phosphorylation and inhibit ERK phosphorylation. Interestingly, NAC, which scavenges ROS, reversed the MMP decline, DNA damage, JNK phosphorylation activation, and ERK phosphorylation inhibition caused by DDH-1. Overall, these findings provide evidence that the eIF4E/eIF4G interaction inhibitors DDH-1 induces DNA damage and apoptosis in human lung cancer A549 cells. (C) 2020 Elsevier B.V. All rights reserved.

Do you like my blog? If you like, you can also browse other articles about this kind. Thanks for taking the time to read the blog about 120-78-5, Quality Control of 2,2-Dithiobis(benzothiazole).

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

Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate55981-09-4, Name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, SMILES is CC(OC1=CC=CC=C1C(NC2=NC=C([N+]([O-])=O)S2)=O)=O, belongs to thiazoles compound. In a article, author is Yanik, Hulya, introduce new discover of the category.

Synthesis, cytotoxic activities and molecular modeling studies of some 2-aminonaphtho[2,3-d][1,3]thiazole-4,9-dione derivatives

Quinones, especially 1,4-naphthoquinones, are one of the most significant and widely distributed phytochemical groups in nature. 1,4-Naphthoquinones and their synthetic derivatives are found to possess remarkable cytotoxic activities. In this study, a series of 2-aminonaphtho[2,3-d][1,3]thiazole-4,9-dione derivatives were synthesized and their structures were verified with spectral analysis. In vitro cytotoxic activities of the synthesized compounds were evaluated by using MTT assay against MKN-45 (Human Gastric cancer), MDA-MB-231 (Human Breast cancer) and HeLa (Human Cervical cancer) cell lines. Among the synthesized compounds, 3d inhibited MDA-MB-cell proliferation with an IC50 value of 0.276 mu M. Compound 3a inhibited HeLa and MKN-45 cell proliferation with IC50 values of 0.336 mu M and 8.769 mu M, respectively. Compound 3b inhibited HELA cell proliferation with an IC50 value of 0.269 mu M. Molecular docking results suggest that the ligands may bind to the hDNA TopoII beta binding pocket and partially exert their effects. These results propose that 2-aminonaphtho[2,3-d]thiazole-4,9-dion core has important biological effects and further explorations are worthwhile. (C)2020 ACG Publication. All right reserved.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions. you can also check out more blogs about 55981-09-4. Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 55981-09-4, Name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, molecular formula is C12H9N3O5S, belongs to thiazoles compound. In a document, author is Gomori, Kamilla, introduce the new discover, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

Cardioprotective Effect of Novel Matrix Metalloproteinase Inhibitors

Background: We recently developed novel matrix metalloproteinase-2 (MMP-2) inhibitor small molecules for cardioprotection against ischemia/reperfusion injury and validated their efficacy in ischemia/reperfusion injury in cardiac myocytes. The aim of the present study was to test our lead compounds for cardioprotection in vivo in a rat model of acute myocardial infarction (AMI) in the presence or absence of hypercholesterolemia, one of the major comorbidities affecting cardioprotection. Methods: Normocholesterolemic adult male Wistar rats were subjected to 30 min of coronary occlusion followed by 120 min of reperfusion to induce AMI. MMP inhibitors (MMPI)-1154 and -1260 at 0.3, 1, and 3 mu mol/kg, MMPI-1248 at 1, 3, and 10 mu mol/kg were administered at the 25th min of ischemia intravenously. In separate groups, hypercholesterolemia was induced by a 12-week diet (2% cholesterol, 0.25% cholic acid), then the rats were subjected to the same AMI protocol and single doses of the MMPIs that showed the most efficacy in normocholesterolemic animals were tested in the hypercholesterolemic animals. Infarct size/area at risk was assessed at the end of reperfusion in all groups by standard Evans blue and 2,3,5-triphenyltetrazolium chloride (TTC) staining, and myocardial microvascular obstruction (MVO) was determined by thioflavine-S staining. Results: MMPI-1154 at 1 mu mol/kg, MMPI-1260 at 3 mu mol/kg and ischemic preconditioning (IPC) as the positive control reduced infarct size significantly; however, this effect was not seen in hypercholesterolemic animals. MVO in hypercholesterolemic animals decreased by IPC only. Conclusions: This is the first demonstration that MMPI-1154 and MMPI-1260 showed a dose-dependent infarct size reduction in an in vivo rat AMI model; however, single doses that showed the most efficacy in normocholesterolemic animals were abolished by hypercholesterolemia. The further development of these promising cardioprotective MMPIs should be continued with different dose ranges in the study of hypercholesterolemia and other comorbidities.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 55981-09-4. Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

In an article, author is Mondal, Ashaparna, once mentioned the application of 120-78-5, Quality Control of 2,2-Dithiobis(benzothiazole), Name is 2,2-Dithiobis(benzothiazole), molecular formula is C14H8N2S4, molecular weight is 332.4867, MDL number is MFCD00022874, category is thiazoles. Now introduce a scientific discovery about this category.

DNA targeting half sandwich Ru(ii)-p-cymene-N boolean AND N complexes as cancer cell imaging and terminating agents: influence of regioisomers in cytotoxicity

For diagnosing and annihilating cancer in the human body, herein, we have adopted a one pot convenient synthetic protocol to synthesize a library of half sandwich Ru(ii)-p-cymene-N<^>N complexes under continuous sonication and isolated their regioisomers by preparative thin layer chromatography followed by justification of stability using DFT. The present work has resulted in a library of ruthenium arene complexes and their isolated regioisomers following environmentally benign green processes and their screening of anticancer activity in terms of cytotoxicity and selectivity against cancer cell lines where [(eta(6)-p-cymene)RuCl{2-(5,6-dichloro-1H-benzo[d]imidazole-2-yl)quinolone}] (11j) has been elicited to be significantly more potent as well as selective in Caco-2 and HeLa cell lines than the normal HEK-293 cell line compared to cisplatin and it has even shown marked cytotoxicity against the more aggressive HT-29 colorectal cancer cell line being capable of producing oxidative stress or arresting the cell cycle. Moreover, these types of Ru(ii)-arene complexes exhibited excellent binding efficacy with DNA and the compounds [(eta(6)-p-cymene)RuCl{5-chloro-2-(6-(4-chlorophenyl)pyridin-2-yl)benzo[d]thiazole}]PF6 (8l4), [(eta(6)-p-cymene)Ru-2-(6-(benzofuran-2-yl)pyridin-2-yl)-5-chlorobenzo[d]thiazole (8l9) and [(eta(6)-p-cymene)RuCl{2-(6-nitro-1H-benzo[d]imidazol-2-yl)quinolone}]Cl (11f ‘) and might be applied for cancer theranostic treatment due to their good fluorescence properties and remarkable potency.

If you are interested in 120-78-5, you can contact me at any time and look forward to more communication. Quality Control of 2,2-Dithiobis(benzothiazole).

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

In an article, author is Duan, Ya-bin, once mentioned the application of 120-78-5, Recommanded Product: 120-78-5, Name is 2,2-Dithiobis(benzothiazole), molecular formula is C14H8N2S4, molecular weight is 332.4867, MDL number is MFCD00022874, category is thiazoles. Now introduce a scientific discovery about this category.

Regulation of High-Altitude Hypoxia on the Transcription of CYP450 and UGT1A1 Mediated by PXR and CAR

Little is known about what roles the pregnane X receptor (PXR) and constitutive androstane receptor (CAR) play in drug metabolism in high-altitude hypoxia. Likewise, the potential interaction of nuclear receptors and drug metabolism enzymes during drug metabolism of high-altitude hypoxia is not fully understood. In this work, we investigated the effects of high-altitude hypoxia on transcriptional regulation of cytochrome P450 (CYP450) and UDP-glucuronosyltransferase 1A1 (UGT1A1) genes mediated by PXR and CAR proteins. The protein and mRNA expressions of CYP450, UGT1A1, PXR, and CAR were determined by enzyme-linked immunosorbent assay and qPCR in rats and HepG2 cell lines under hypoxia. Hypoxia potently inhibited the CYP450 isoforms, UGT1A1, PXR, and CAR protein and mRNA expression. To clarify whether PXR and CAR regulate various genes involved in drug metabolism of high-altitude hypoxia, we investigated the expression of CYP1A2, CYP2C9, CYP2E1, CYP3A4, and UGT1A1 using a dual-luciferase reporter assay after treatment with Ketoconazole (KCZ) and Retinoic acid (RA), or silenced PXR and CAR gene expression. In HepG2 cells, hypoxia, KCZ, and RA inhibited CYP450 isoforms and UGT1A1 expression. Activation of PXR and CAR in cells treated with 6-(4-chlorophenyl)-imidazo (2,1-b) thiazole-5-carbaldehyde (CITCO) and rifampicin (Rif) resulted in the enhancement of CYP450 isoforms, UGT1A1, PXR, and CAR. In contrast, this effect was not observed under hypoxia. Taken together, our results suggest that hypoxia inhibits CYP1A2, CYP2C9, CYP2E1, CYP3A4, and UGT1A1 expressionviathe PXR and CAR regulatory pathway.

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