121952-97-4Relevant academic research and scientific papers
Proapoptotic effects of novel thiazole derivative on human glioma cells
Finiuk, Nataliya,Klyuchivska, Olha,Ivasechko, Iryna,Hreniukh, Volodymyr,Ostapiuk, Yuriy,Shalai, Yaryna,Panchuk, Rostyslav,Matiychuk, Vasyl,Obushak, Mykola,Stoika, Rostyslav,Babsky, Andriy
, p. 27 - 37 (2019)
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
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
Tupys, Andrii,Kalembkiewicz, Jan,Bazel, Yaroslav,Zapa?a, Lidia,Dranka, Maciej,Ostapiuk, Yurii,Tymoshuk, Oleksandr,Wo?nicka, El?bieta
, p. 722 - 733 (2017)
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
Synthesis, structural characterization and thermal studies of a novel reagent 1-[(5-benzyl-1,3-thiazol-2-yl)diazenyl]naphthalene-2-ol
Tupys, Andrii,Kalembkiewicz, Jan,Ostapiuk, Yurii,Matiichuk, Vasyl,Tymoshuk, Oleksandr,Wo?nicka, El?bieta,Byczyński, ?ukasz
, p. 2233 - 2242 (2017)
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:
COMPOUNDS AND USES THEREOF
-
, (2020/10/20)
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.
COMPOUNDS AND USES THEREOF
-
, (2019/10/15)
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.
SMALL MOLECULE ACTIVATORS OF NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE (NAMPT) AND USES THEREOF
-
Paragraph 01096, (2018/08/03)
Provided herein are small molecule activators of Nicotinamide Phosphoribosyltransferase (NAMPT), compositions comprising the compounds, and methods of using the compounds and compositions.
Synthesis and antitumor activities of new n-(5-benzylthiazol-2-yl)-2-(heteryl-5-ylsulfanyl)-acetamides
Ostapiuk, Yu. V.,Frolov,Vasylyschyn, R. Ya.,Matiychuk
, p. 59 - 71 (2018/05/15)
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,
Antineoplastic activity of novel thiazole derivatives
Finiuk,Hreniuh,Ostapiuk, Yu.V.,Matiychuk,Frolov,Obushak,Stoika,Babsky
, p. 135 - 146 (2017/08/07)
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
Identification of KPNB1 as a Cellular Target of Aminothiazole Derivatives with Anticancer Activity
Kim, Yong-Hak,Ha, Siyoung,Kim, Jungwon,Ham, Seung Wook
supporting information, p. 1406 - 1409 (2016/07/16)
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.
Design, synthesis, and biological evaluation of aminothiazole derivatives against the fungal pathogens Histoplasma capsulatum and Cryptococcus neoformans
Khalil, Ahmed,Edwards, Jessica A.,Rappleye, Chad A.,Tjarks, Werner
, p. 532 - 547 (2015/01/30)
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.
