Category: thiazolidine

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Hybridized quinoline derivatives as anticancer agents: Design, synthesis, biological evaluation and molecular docking

Objective: Conjugating quinolones with different bioactive pharmacophores to obtain potent anticancer active agents. Methods: Fused pyrazolopyrimidoquinolines 3a-d, Schiff bases 5, 6a-e, two hybridized systems: pyrazolochromenquinoline 7 and pyrazolothiazolidinquinoline 8, different substituted thiazoloquinolines 13-15 and thiazolo[3,2-a]pyridine derivatives 16a-c were synthesized. Their chemical structures were characterized through spectral and elemental analysis, cytotoxic activity on five cancer cell lines, caspase-3 activation, tubulin polymerization inhibition and cell cycle analysis were evaluated. Results: Four compounds 3b, 3d, 8 and 13 showed potent activity than doxorubicin on HCT116 and three compounds 3b, 3d and 8 on HEPG2. These promising derivatives showed increase in the level of caspase-3. The trifloromethylphenyl derivatives of pyrazolopyrimidoquinolines 3b and 3d showed considerable tubulin polymerization inhibitory activity. Both compounds arrested cell cycle at G2/M phase and induced apoptosis. Conclusion: Compounds 3b and 3d can be considered as promising anticancer active agents with 70% of colchicine activity on tubulin polymerization inhibition and represent hopeful leads that deserve further investigation and optimization.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H445N | ChemSpider

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Synthesis and evaluation of anticonvulsant activities of 5-benzylidene-2-(5-methylisoxazol-3-ylimino)thiazolidin-4-one derivatives

Fifteen new 5-benzylidene-2-(5-methylisoxazol-3-ylimino)thiazolidin-4-one derivatives (4-18) were synthesized and evaluated for their preliminary anticonvulsant activity and neurotoxicity by using the maximal electroshock (MES) and rotarod tests. The structures of synthesized compounds were established by IR,1H NMR,13C NMR and mass spectral data. Among the compounds studied, 5-(3-fluorobenzylidene)-2-(5-methylisoxazol-3-ylimino)thiazolidin-4-one (8) was the most potent compound, with a median effective dose of 43.9 mg/kg and a high protective index (PI) of more than 11.1 after intraperitoneal administration in mice. Compound 8 showed significant oral activity against MES-induced seizures in mice, with an ED50 of 84.2 mg/kg and a PI above 11.8. These results demonstrate that compound 8 is safer than the commercially drugs.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H478N | ChemSpider

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. Quality Control of 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrile. Introducing a new discovery about 1055361-35-7, Name is 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrile

Design, synthesis and biological evaluation of 4-anilinoquinoline derivatives as novel potent tubulin depolymerization agents

A series of novel 4-anilinoquinoline derivatives were synthesized and evaluated for their antiproliferative activities. Among them, 14h exhibited the most potent cytotoxic activity with IC50 values ranging from 1.5 to 3.9 nM against all tested cancer cell lines, and showed promising efficacy in multidrug resistant cancer cells. Flow cytometry assay, immune-fluorescence staining, microtubule dynamics assays and competition assays with EBI identified that 14h was a novel tubulin depolymerization agent by binding to the colchicine site. Importantly, in vivo efficacy evaluation of HCT116 xenograft model, 14h showed efficient antitumor activity without significant loss in body weight. All the results indicated that 14h could be a promising candidate for the treatment of cancer.

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.Quality Control of 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrile, you can also check out more blogs about1055361-35-7

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Quinuclidine – Wikipedia,
Quinuclidine | C7H950N | ChemSpider

Chemistry is traditionally divided into organic and inorganic chemistry. Safety of Thiazolidin-2-one, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 2682-49-7

Amines having secondary aliphatic amino groups

The present invention relates to novel amides having secondary amino groups, a process for preparing them, adducts of these amines and their uses. The amides can be prepared in a simple way from readily available starting materials. They and their adducts have, in particular, a low viscosity and are suitable as constituent of polyurethane and polyurea compositions having excellent processability and high flexibility, and also as constituent of epoxy resin compositions, in particular coatings.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H178N | ChemSpider

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PTP1b inhibition, a promising approach for the treatment of diabetes type II

Background: Diabetes Mellitus (DM), is a metabolic disorder characterized by high blood glucose levels. The main types of diabetes mellitus are Diabetes mellitus type I, Diabetes mellitus type II, gestational diabetes and Diabetes of other etiology. Diabetes type II, the Non Insulin Dependent Type (NIDDM) is the most common type, characterized by the impairment in activation of the intracellular mechanism leading to the insertion and usage of glucose after interaction of insulin with its receptor, known as insulin resistance. Although, a number of drugs have been developed for the treatment of diabetes type II, their ability to reduce blood glucose levels is limited, while several side effects are also observed. Furthermore, none of the market drugs targets the enhancement of the action of the intracellular part of insulin receptor or recuperation of the glucose transport mechanism in GLUT4 dependent cells. The Protein Tyrosine Phosphatase (PTP1b) is the main enzyme involved in insulin receptor desensitization and has become a drug target for the treatment of Diabetes type II. Several PTP1b inhibitors have already been found, interacting with the binding site of the enzyme, surrounding the catalytic amino acid Cys215 and the neighboring area or with the allosteric site of the enzyme, placed at a distance of 20 A from the active site, around Phe280. However, the research continues for finding more potent inhibitors with increased cell permeability and specificity. Objective: The aim of this review is to show the attempts made in developing of Protein Tyrosine Phosphatase (PTP1b) inhibitors with high potency, selectivity and bioavailability and to sum up the indications for favorable structural characteristics of effective PTP1b inhibitors. Methods: The methods used include a literature survey and the use of Protein Structure Databanks such as PuBMed Structure and RCSB and the tools they provide. Conclusion: The research for finding PTP1b inhibitors started with the design of molecules mimicking the Tyrosine substrate of the enzyme. The study revealed that an aromatic ring connected to a polar group, which preferably enables hydrogen bond formation, is the minimum requirement for small inhibitors binding to the active site surrounding Cys215. Molecules bearing two hydrogen bond donor/acceptor (Hb d/a) groups at a distance of 8.5-11.5 A may form more stable complexes, interacting simultaneously with a secondary area A2. Longer molecules with two Hb d/a groups at a distance of 17 A or 19 A may enable additional interactions with secondary sites (B and C) that confer stability as well as specificity. An aromatic ring linked to polar or Hb d/a moieties is also required for allosteric inhibitors. A lower distance between Hb d/a moieties, around 7.5 A may favor allosteric interaction. Permanent inhibition of the enzyme by oxidation of the catalytic Cys215 has also been referred. Moreover, covalent modification of Cys121, placed near but not inside the catalytic pocket has been associated with permanent inhibition of the enzyme.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H275N | ChemSpider

Synthetic Route of 2682-49-7, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 2682-49-7, molcular formula is C3H5NOS, introducing its new discovery.

Synthesis and biological evaluation of indole-2-carbohydrazides and thiazolidinyl-indole-2-carboxamides as potent tubulin polymerization inhibitors

A new series of N?-(substituted phenyl)-5-chloro/iodo-3-phenyl-1H-indole-2-carbohydrazide (5, 6) and N-[2-(substituted phenyl)-4-oxo-1,3-thiazolidin-3-yl]-5-iodo/chloro-3-phenyl-1H-indole-2-carboxamide (7, 8) derivatives were synthesized and evaluated for their anticancer properties. Compounds 5a and 6b, selected as prototypes by the National Cancer Institute for screening against the full panel of 60 human tumor cell lines at a minimum of five concentrations at 10-fold dilutions, demonstrated remarkable antiproliferative activity against leukemia, non-small cell lung cancer, colon cancer, central nervous system (CNS) cancer, melanoma, ovarian cancer, renal cancer, and breast cancer (MCF-7) cell lines with GI50 values < 0.4 muM. A subset of the compounds was then tested for their potential to inhibit tubulin polymerization. Compounds 6f and 6g showed significant cytotoxicity at the nM level on MCF-7 cells and exhibited significant inhibitory activity on tubulin assembly and colchicine binding at about the same level as combretastatin A-4. Finally, docking calculations were performed to identify the binding mode of these compounds. Group 5 and 6 compounds interacted with the colchicine binding site through hydrophobic interactions similar to those of colchicine. These compounds with antiproliferative activity at high nanomolar concentration can serve as scaffolds for the design of novel microtubule targeting agents. The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 2682-49-7 is helpful to your research. Synthetic Route of 2682-49-7

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Quinuclidine – Wikipedia,
Quinuclidine | C7H340N | ChemSpider

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Computed Properties of C3H5NOS, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 2682-49-7, name is Thiazolidin-2-one. In an article£¬Which mentioned a new discovery about 2682-49-7

Studies on inclusion complexes of 2-[4-(5′-benzylidene-4′-oxo-3′-phenyl thiazolidinyl-2′-imino)benzoyl]aminoimino-5-benzylidene-3-phenyl-4-thiazolidinone with ss-cyclodextrin

Thiazolidinones and its derivatives are good pharamacores and showing wide spectrum of fungicidal, antibacterial and tubercolostic activities.A series of 2-[4-(5′-benzylidene-4′-oxo-3′-phenylthiazolidinyl-2′-imino) benzoyl] aminoimino-5-benzylidene-3-phenyl-4-thiazolidinone have been synthesized starting from p-Aminobenzoic acid.To enhance the solubility of these synthesized compounds,the inclusion complexes were prepared with ss-cyclodextrin.The synthesis of compounds and their inclusion complexes have been ascertained from the changes in spectral characteristics and their analytical data.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H289N | ChemSpider

Reference of 7025-19-6, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.7025-19-6, Name is 3-(4-Oxo-2-thioxothiazolidin-3-yl)propanoic acid, molecular formula is C6H7NO3S2. In a Article£¬once mentioned of 7025-19-6

Anticancer Activity of Copper Complex of (4R)-(-)-2-Thioxo-4-thiazolidinecarboxylic Acid and 3-Rhodaninepropionic Acid on Prostate and Breast Cancer Cells by Fluorescent Microscopic Imaging

Copper complexes with strong anticancer activity are promising new drugs for treatment of patients with metastatic cancer. Copper 8-hydroxyquinoline-2-carboxaldehyde-thiosemicarbazide (CuHQTS) and copper 8-hydroxyquinoline-2-carboxaldehyde-4,4-dimethyl-3-thiosemicarbazide (CuHQDMTS) were found to have strong anticancer activity against cisplatin-resistant neuroblastoma cells and prostate cancer cells. This study aimed to synthesize and characterize two new anticancer copper complexes, copper complex of (4R)-(?)-2-Thioxo-4-thiazolidinecarboxylic acid (CuTTDC), and copper complex of 3-Rhodaninepropionic acid-copper complex (CuRDPA). Cell growth inhibition and cytotoxicity of CuTTDC and CuRDPA on prostate and breast cancer cells were evaluated with Cell Counting Kits-8 (CCK8) assay and fluorescent microscopic imaging respectively. Strong anticancer activity of CuTTDC and CuRDPA was demonstrated by growth inhibition and cytotoxicity of prostate and breast cancer cells treated with these two copper complexes, supporting further investigation of potential use of these two new anticancer complexes for treatment of prostate and breast cancer metastasis.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H822N | ChemSpider

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Recommanded Product: 76186-04-4, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 76186-04-4, Name is (S)-4-Isopropylthiazolidine-2-thione, molecular formula is C6H11NS2

Synthesis and Incorporation of the First Polyketide Synthase Free Intermediate in Monocerin Biosynthesis

Enzyme essential: Feeding studies with Dreschlera ravenelii show that labeled dihydroisocoumarin 1 is metabolized into monocerin (2) in exceptionally high levels. These results provide evidence for the role of 1 as the first enzyme-free intermediate in the monocerin biosynthesis pathway and, thus, as the final product of the polyketide synthase (PKS) catalyzed part of the pathway. Compound 1 may therefore be of use in further studies to isolate and sequence the monocerin PKS gene.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H715N | ChemSpider

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Quality Control of Thiazolidin-2-one, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 2682-49-7, name is Thiazolidin-2-one. In an article£¬Which mentioned a new discovery about 2682-49-7

Synthesis and Biological Evaluation of Novel 5-Oxo-1-Phenylpyrrolidine-3-Carboxylic Acid Analogs

A number of 5-oxo-1-phenyl-4-(substituted methyl) pyrrolidine-3-carboxylic acid derivatives bearing pyrrolidine ring and methylamino residues in their structure were synthesized as potential antibacterial drugs. The chemical structures of all the compounds were established by their UV-Vis absorption spectroscopy, IR, 1 H, 13 C NMR and mass spectroscopy. The in vitro antibacterial screening of all novel compounds was done against gram-positive Staphylococcus aureus, Bacillus subtilis and gram-negative Pseudomonas aeruginosa. The results revealed that compounds 5d, e, f and g showed moderate to good activity against the tested microbes.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H264N | ChemSpider