- Proapoptotic effects of novel thiazole derivative on human glioma cells
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The aim of the present study was to investigate the antiproliferative and proapoptotic actions of N-(5-benzyl-1,3-thiazol-2-yl)-3,5-dimethyl-1-benzofuran-2-carboxamide derivative (compound 5) in glioma cells in comparison with the actions of temozolomide
- Finiuk, Nataliya,Klyuchivska, Olha,Ivasechko, Iryna,Hreniukh, Volodymyr,Ostapiuk, Yuriy,Shalai, Yaryna,Panchuk, Rostyslav,Matiychuk, Vasyl,Obushak, Mykola,Stoika, Rostyslav,Babsky, Andriy
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- 1-[(5-Benzyl-1,3-thiazol-2-yl)diazenyl]naphthalene-2-ol: X-ray structure, spectroscopic characterization, dissociation studies and application in mercury(II) detection
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A new thiazolylazo reagent, 1-[(5-benzyl-1,3-thiazol-2-yl)diazenyl]naphthalene-2-ol, has been synthesized for the first time. Single crystals of the azo dye were grown from a saturated solution by the vapour diffusion technique. The compound was analyzed
- Tupys, Andrii,Kalembkiewicz, Jan,Bazel, Yaroslav,Zapa?a, Lidia,Dranka, Maciej,Ostapiuk, Yurii,Tymoshuk, Oleksandr,Wo?nicka, El?bieta
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- Synthesis, structural characterization and thermal studies of a novel reagent 1-[(5-benzyl-1,3-thiazol-2-yl)diazenyl]naphthalene-2-ol
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A new thiazolylazo reagent 1-[(5-benzyl-1,3-thiazol-2-yl)diazenyl]naphthalene-2-ol has been synthesized via arylation of acrolein and further diazotization and diazocoupling with 2-naphthol. The chemical structure of the compound was confirmed by IR, NMR:
- Tupys, Andrii,Kalembkiewicz, Jan,Ostapiuk, Yurii,Matiichuk, Vasyl,Tymoshuk, Oleksandr,Wo?nicka, El?bieta,Byczyński, ?ukasz
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- COMPOUNDS AND USES THEREOF
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The present invention features compounds useful in the treatment of neurological disorders and primary brain cancer. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders and primary brain cancer.
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(2020/10/20)
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- COMPOUNDS AND USES THEREOF
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The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
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Page/Page column 315-316
(2019/10/15)
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- SMALL MOLECULE ACTIVATORS OF NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE (NAMPT) AND USES THEREOF
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Provided herein are small molecule activators of Nicotinamide Phosphoribosyltransferase (NAMPT), compositions comprising the compounds, and methods of using the compounds and compositions.
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Paragraph 01096
(2018/08/03)
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- Synthesis and antitumor activities of new n-(5-benzylthiazol-2-yl)-2-(heteryl-5-ylsulfanyl)-acetamides
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Aim. Synthesis of a series of new N-(5-benzyl-thiazol-2-yl)-2-(heteryl-5-ylsulfanyl)-acetamides and study of their anticancer activity. Methods. Organic synthesis, analytical and spectral methods, pharmacological screening. Results. [2-chloro-N-(5-aryl-1,
- Ostapiuk, Yu. V.,Frolov,Vasylyschyn, R. Ya.,Matiychuk
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- Antineoplastic activity of novel thiazole derivatives
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The development of novel efficient substances for anticancer chemotherapy is an important problem of medicinal chemistry. Aim. To evaluate the level of cytotoxic action of novel thiazole derivatives towards tumor cell lines of different origin. Methods. F
- Finiuk,Hreniuh,Ostapiuk, Yu.V.,Matiychuk,Frolov,Obushak,Stoika,Babsky
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p. 135 - 146
(2017/08/07)
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- Identification of KPNB1 as a Cellular Target of Aminothiazole Derivatives with Anticancer Activity
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We found that aminothiazole derivative (E)-N-(5-benzylthiazol-2-yl)-3-(furan-2-yl)acrylamide (1) has strong anticancer activity, and undertook proteomics approaches to identify the target protein of compound 1, importin β1 (KPNB1). A competitive binding assay using fluorescein-labeled 1 showed that 1 has strong binding affinity for KPNB1 (Kd: ~20 nm). Furthermore, through western blotting assays for KPNB1, KPNA2, EGFR, ErbB2, and STAT3, we confirmed that 1 has inhibitory effects on the importin pathway. KPBN1 appears to be overexpressed in several cancer cells, and siRNA-induced inhibition of KPNB1 shows significant inhibition of cancer cell proliferation, while leaving non-cancerous cells unaffected. Therefore, compound 1 is a promising new lead for the development of KPNB1-targeted anticancer agents. Fluorescein-labeled 1 could be a useful quantitative probe for the development of novel KPNB1 inhibitors.
- Kim, Yong-Hak,Ha, Siyoung,Kim, Jungwon,Ham, Seung Wook
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supporting information
p. 1406 - 1409
(2016/07/16)
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- Identification of Aminoimidazole and Aminothiazole Derivatives as Src Family Kinase Inhibitors
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Src family kinases (SFKs) are a family of non-receptor tyrosine kinases (TKs) implicated in the regulation of many cellular processes. The aberrant activity of these TKs has been associated with the growth and progression of cancer. In particular, c-Src i
- Francini, Cinzia Maria,Fallacara, Anna Lucia,Artusi, Roberto,Mennuni, Laura,Calgani, Alessia,Angelucci, Adriano,Schenone, Silvia,Botta, Maurizio
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p. 2027 - 2041
(2015/12/23)
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- Design, synthesis, and biological evaluation of aminothiazole derivatives against the fungal pathogens Histoplasma capsulatum and Cryptococcus neoformans
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Invasive fungal disease constitutes a growing health burden and development of novel antifungal drugs with high potency and selectivity against new fungal molecular targets are urgently needed. Previously, an aminothiazole derivative, designated as 41F5, was identified in our laboratories as highly active against Histoplasma yeast (MIC50 0.4-0.8 μM) through phenotypic high-throughput screening of a commercial library of 3600 purine mimicking compounds (Antimicrob. Agents Chemother. 2013, 57, 4349). Consequently, 68 analogues of 41F5 were designed and synthesized or obtained from commercial sources and their MIC50s of growth inhibition were evaluated in Histoplasma capsulatum to establish a basic structure-activity-relationship (SAR) for this potentially new class of antifungals. The growth inhibiting potentials of smaller subsets of this library were also evaluated in Cryptococcus neoformans and human hepatocyte HepG2 cells, the latter to obtain selectivity indices (SIs). The results indicate that a thiazole core structure with a naphth-1-ylmethyl group at the 5-position and cyclohexylamide-, cyclohexylmethylamide-, or cyclohexylethylamide substituents at the 2-position caused the highest growth inhibition of Histoplasma yeast with MIC50s of 0.4 μM. For these analogues, SIs of 92 to >100 indicated generally low host toxicity. Substitution at the 3- and 4-position decreased antifungal activity. Similarities and differences were observed between Histoplasma and Cryptococcus SARs. For Cryptococcus, the naphth-1-ylmethyl substituent at the 5-position and smaller cyclopentylamide- or cyclohexylamide groups at the 2-position were important for activity. In contrast, slightly larger cyclohexylmethyl- and cyclohexylethyl substituents markedly decreased activity.
- Khalil, Ahmed,Edwards, Jessica A.,Rappleye, Chad A.,Tjarks, Werner
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p. 532 - 547
(2015/01/30)
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- A convenient method for the synthesis of 2-[(5-benzyl-1,3-thiazol-2-yl) imino]-1,3-thiazolidin-4-one derivatives
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It was found that the reaction of 2-chloroacetamido/chloropropioamido-5- benzylthiazole with potassium thiocyanate gave, via rearrangement, 2-[(5-benzyl-1,3-thiazol-2-yl)imino]-1,3-thiazolidin-4-ones.
- Ostapiuk, Yuri V.,Obushak, Mykola D.,Matiychuk, Vasyl S.,Naskrent, Marek,Gzella, Andrzej K.
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p. 543 - 545
(2012/03/10)
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- Synthesis of 2-azido-1,3-thiazoles as 1,2,3-triazole precursors
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By diazotization of 2-aminothiazoles and reaction with sodium azide, the derivatives of 2-azidothiazole were synthesized. Conditions of diazotization were selected according to the nature of a substituent in thiazoles. 2-Azidothiazole derivatives were studied in the base-catalysed condensation reactions with activated methylenic compounds to yield new 1-(1,3-thiazol-2-yl)- 1H-1,2,3-triazole-4-carboxylic acids.
- Pokhodylo, Nazariy T.,Savka, Roman D.,Pidlypnyi, Nazar I.,Matiychuk, Vasyl S.,Obushak, Mykola D.
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scheme or table
p. 391 - 399
(2010/03/30)
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- Discovery and potency optimization of 2-amino-5-arylmethyl-1,3-thiazole derivatives as potential therapeutic agents for prostate cancer
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A new chemical series was identified via high-throughput screening as having antiproliferative activity on DU-145 human prostate carcinoma cell line (hit compound potency - 2.9 μM). Medicinal chemistry optimization of two peripheral diversity vectors of t
- Krasavin, Mikhail,Karapetian, Ruben,Konstantinov, Igor,Gezentsvey, Yuri,Bukhryakov, Konstantin,Godovykh, Elena,Soldatkina, Olga,Lavrovsky, Yan,Sosnov, Andrei V.,Gakh, Andrei A.
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experimental part
p. 420 - 427
(2009/11/30)
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- MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
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The present invention relates to modulators of ATP-Binding Cassette ("ABC") transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator ("CFTR"), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators (I) or a pharmaceutically acceptable salt thereof, wherein: Ht is a 5-membered heteroaromatic ring containing 1-4 heteroatoms selected from O, S, N or NH, wherein said ring is optionally fused to a 6-membered monocyclic or 10-membered bicyclic carbocyclic or heterocyclic, aromatic or non-aromatic ring, wherein Ht is optionally substituted with w occurrences of -WRw, wherein w is 0-5; ring A is 3-7 membered monocyclic ring having 0-3 heteroatoms selected from O, S, N, or NH, wherein ring A is optionally substituted with q occurrences of QRQ; ring B is optionally fused to 5-6 membered carbocyclic or heterocyclic, aromatic or non-aromatic ring .
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(2010/02/13)
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- Heterocyclic Syntheses on the Basis of Anionarylation Products of Unsaturated Compounds. I. 2-Amino-5-arylmethyl-1,3-thiazoles
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3-Aryl-2-chloropropionaldehydes have been prepared by reactions of arenediazonium chlorides with acrolein in the presence of CuCl2. Reactions of these aldehydes with thiourea provide a convenient route to difficultly accessible 2-amino-5-arylme
- Obushak,Matiichuk,Ganushchak
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p. 1010 - 1013
(2007/10/03)
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- Substituted imidazo[2,1-b]thiazoles from 2-aminothiazoles and α-bromo ketones: Efficient preparation and proof of structure
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The salts formed from α-aminothiazoles and α-bromo ketones (RCOCH2Br) have been basified, and the products converted into amides. Examination of the amides established that they are 2-acylimino-2,3- dihydrothiazoles rather than 2-acylaminothiaz
- Meakins, G. Denis,Musk, Sally R. R.,Robertson, Colin A.,Woodhouse, Lee S.
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p. 643 - 648
(2007/10/02)
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