排序方式: 共有64条查询结果,搜索用时 15 毫秒
1.
Iryna Ivasechko Ihor Yushyn Piotr Roszczenko Julia Senkiv Nataliya Finiuk Danylo Lesyk Serhii Holota Robert Czarnomysy Olga Klyuchivska Dmytro Khyluk Nataliya Kashchak Andrzej Gzella Krzysztof Bielawski Anna Bielawska Rostyslav Stoika Roman Lesyk 《Molecules (Basel, Switzerland)》2022,27(19)
Novel pyridine-thiazole hybrid molecules were synthesized and subjected to physico-chemical characterization and screening of their cytotoxic action towards a panel of cell lines derived from different types of tumors (carcinomas of colon, breast, and lung, glioblastoma and leukemia), and normal human keratinocytes, for comparison. High antiproliferative activity of the 3-(2-fluorophenyl)-1-[4-methyl-2-(pyridin-2-ylamino)-thiazol-5-yl]-propenone 3 and 4-(2-{1-(2-fluorophenyl)-3-[4-methyl-2-(pyridin-2-ylamino)-thiazol-5-yl]-3-oxopropylsulfanyl}-acetylamino)-benzoic acid ethyl ester 4 was revealed. The IC50 of the compound 3 in HL-60 cells of the acute human promyelocytic leukemia was 0.57 µM, while in the pseudo-normal human cell lines, the IC50 of this compound was >50 µM, which suggests that the compounds 3 and 4 might be perspective anticancer agents. The detected selectivity of the derivatives 3 and 4 for cancer cell lines inspired us to study the mechanisms of their cytotoxic action. It was shown that preincubation of tumor cells with Fluzaparib (inhibitor of PARP1) reduced the cytotoxic activity of the derivatives 3 and 4 by more than twice. The ability of these compounds to affect DNA nativity and cause changes in nucleus morphology allows for the suggestion that the mechanism of action of the novel pyridine-thiazole derivatives might be related to inducing the genetic instability in tumor cells. 相似文献
2.
Shubham Deolka Ramadoss Govindarajan Serhii Vasylevskyi Michael C. Roy Julia R. Khusnutdinova Eugene Khaskin 《Chemical science》2022,13(44):12971
We describe a “ligand-free” Ni-catalyzed perfluoroalkylation of heteroarenes to produce a diverse array of trfiluoromethyl, pentafluoroethyl and heptafluoropropyl adducts. Catalysis proceeds at room temperature via a radical pathway. The catalytic protocol is distinguished by its simplicity, and its wide scope demonstrates the potential in the late-stage functionalization of drug analogues and peptides.A ligand-free, room temperature, Ni-catalyzed perfluoroalkylation of heteroarenes produced a diverse array of polyfluorinated adducts; potential in the late-stage functionalization of drugs and peptides is also demonstrated. 相似文献
3.
Serhii Krykun Maksym Dekhtiarenko David Canevet Vincent Carr Frdric Aubriet Eric Levillain Magali Allain Zoia Voitenko Marc Sall Sbastien Goeb 《Angewandte Chemie (International ed. in English)》2020,59(2):716-720
Developing methodologies for on‐demand control of the release of a molecular guest requires the rational design of stimuli‐responsive hosts with functional cavities. While a substantial number of responsive metallacages have already been described, the case of coordination‐tweezers has been less explored. Herein, we report the first example of a redox‐triggered guest release from a metalla‐assembled tweezer. This tweezer incorporates two redox‐active panels constructed from the electron‐rich 9‐(1,3‐dithiol‐2‐ylidene)fluorene unit that are facing each other. It dimerizes spontaneously in solution and the resulting interpenetrated supramolecular structure can dissociate in the presence of an electron‐poor planar unit, forming a 1:1 host–guest complex. This complex dissociates upon tweezer oxidation/dimerization, offering an original redox‐triggered molecular delivery pathway. 相似文献
4.
Dr. Serhii Krykun Dr. Muriel Durandetti 《European journal of organic chemistry》2023,26(4):e202201393
A convenient and efficient approach for the construction of aryl trifluoromethyl selenoethers from aryl iodides under mild conditions is reported. Electrochemical activation of stable and inexpensive NiBr2bipy (bipy – bipyridine) complex instead of labile Ni(COD)2 (COD – cyclooctadiene) catalyst. [NMe4][SeCF3] is employed as shelf-stable source of SeCF3 fragment. The reaction tolerates a wide range of substrates, including modification of drug-like molecules. Cyclic voltammetry studies allow insight into the reaction mechanism. 相似文献
5.
Serhii A. Liakhov Igor A. Schepetkin Olexander S. Karpenko Hanna I. Duma Nadiia M. Haidarzhy Liliya N. Kirpotina Anastasia R. Kovrizhina Andrei I. Khlebnikov Irina Y. Bagryanskaya Mark T. Quinn 《Molecules (Basel, Switzerland)》2021,26(18)
c-Jun N-terminal kinase (JNK) plays a central role in stress signaling pathways implicated in important pathological processes, including rheumatoid arthritis and ischemia-reperfusion injury. Therefore, inhibition of JNK is of interest for molecular targeted therapy to treat various diseases. We synthesized 13 derivatives of our reported JNK inhibitor 11H-indeno[1,2-b]quinoxalin-11-one oxime and evaluated their binding to the three JNK isoforms and their biological effects. Eight compounds exhibited submicromolar binding affinity for at least one JNK isoform. Most of these compounds also inhibited lipopolysaccharide (LPS)-induced nuclear factor-κB/activating protein 1 (NF-κB/AP-1) activation and interleukin-6 (IL-6) production in human monocytic THP1-Blue cells and human MonoMac-6 cells, respectively. Selected compounds (4f and 4m) also inhibited LPS-induced c-Jun phosphorylation in MonoMac-6 cells, directly confirming JNK inhibition. We conclude that indenoquinoxaline-based oximes can serve as specific small-molecule modulators for mechanistic studies of JNKs, as well as potential leads for the development of anti-inflammatory drugs. 相似文献
6.
Serhii Gryshchuk Massimo Lanza de Cristoforis 《Mathematical Methods in the Applied Sciences》2014,37(12):1755-1771
Let be a bounded open domain of . Let denote the outward unit normal of . We assume that the Steklov problem Δu = 0 in and on has a simple eigenvalue of . Then we consider an annular domain obtained by removing from a small‐cavity size of ε > 0, and we show that under proper assumptions there exists a real valued and real analytic function defined in an open neighborhood of (0,0) in and such that is a simple eigenvalue for the Steklov problem Δu = 0 in and on for all ε > 0 small enough, and such that . Here denotes the outward unit normal of , and δ2,2 ≡ 1 and δ2,n ≡ 0 if n ≥ 3. Then related statements have been proved for corresponding eigenfunctions. Copyright © 2013 John Wiley & Sons, Ltd. 相似文献
7.
The effects of temperature and mobile phase on the retention of aliphatic carboxylic acids in hydrophilic interaction chromatography on zwitterionic stationary phases 下载免费PDF全文
The influence of the mobile phase and temperature, on the retention behavior of seven aliphatic acids (pyruvic, gluconic, 2‐oxoglutaric, tartaric, malic, oxalic, and citric acid) in hydrophilic interaction liquid chromatography on zwitterionic stationary phases with sulfobetaine and phosphorylcholine ligands is investigated. In agreement with the van't Hoff model, most acids show linear ln k versus 1/T plots. However, the retention of structurally symmetrical oxalic and tartaric dicarboxylic acids is almost independent of temperature, or slightly increases at rising temperature. The experimental parameters of the van't Hoff plots suggest positive entropic contributions to the retention of these symmetrical acids, possibly connected with changes in molecular symmetry on their adsorption. The type of the zwitterionic stationary phase and the mobile phase composition (the molar concentration of acetate buffer and the volume fraction of acetonitrile) affect the retention and the selectivity of the separation of the acids. 相似文献
8.
Serhii V. Gryshchuk Sergiy A. Plaksa 《Mathematical Methods in the Applied Sciences》2016,39(11):2939-2952
We consider a commutative algebra over the field of complex numbers with a basis {e1,e2} satisfying the conditions , . Let D be a bounded domain in the Cartesian plane xOy and Dζ={xe1+ye2:(x,y)∈D}. Components of every monogenic function Φ(xe1+ye2) = U1(x,y)e1+U2(x,y)ie1+U3(x,y)e2+U4(x,y)ie2 having the classic derivative in Dζ are biharmonic functions in D, that is, Δ2Uj(x,y) = 0 for j = 1,2,3,4. We consider a Schwarz‐type boundary value problem for monogenic functions in a simply connected domain Dζ. This problem is associated with the following biharmonic problem: to find a biharmonic function V(x,y) in the domain D when boundary values of its partial derivatives ?V/?x, ?V/?y are given on the boundary ?D. Using a hypercomplex analog of the Cauchy‐type integral, we reduce the mentioned Schwarz‐type boundary value problem to a system of integral equations on the real axes and establish sufficient conditions under which this system has the Fredholm property. Copyright © 2015 John Wiley & Sons, Ltd. 相似文献
9.
Halko R Padrón Sanz C Sosa Ferrera Z Santana Rodríguez JJ 《Journal of AOAC International》2006,89(5):1403-1409
A simple and fast analytical method was developed for the determination of benzimidazole fungicides (benomyl, carbendazim, thiabendazole, and fuberidazole) in soil samples. The analytes were extracted from the soil samples by means of conventional microwave-assisted extraction, using the non-ionic surfactants polyoxyethylene 10 lauryl ether (POLE) and oligoethylene glycol monooalkyl ether (Genapol X-080) as extractants. Determinations were made by using liquid chromatography with direct fluorescence detection. The use of an analytical column Symmetry C-18 offered short retention times of analytes without the need of any pH regulators with mobile phase methanol-water (50 + 50, v/v). The best results were obtained using 5% (v/v) POLE as extractant with recoveries of the fungicides in spiked soil samples between 71 and 105%. The results were compared with those obtained when Soxhlet extraction was applied to the same soil samples. 相似文献
10.
Dr. Sergiy V. Zasukha Prof. Dr. Vadim M. Timoshenko Prof. Dr. Andrey A. Tolmachev Valentyna O. Pivnytska Oleksii Gavrylenko Dr. Serhii Zhersh Prof. Dr. Yuriy Shermolovich Dr. Oleksandr O. Grygorenko 《Chemistry (Weinheim an der Bergstrasse, Germany)》2019,25(28):6928-6940
Two novel solid reagents—1-sulfonimidoyl- and 1-sulfamimidoyl-3-methylimidazolium derivatives—for the synthesis of sulfonimidamides and imidosulfuric diamides, respectively, were developed. It is shown that these reagents are very effective in substitution reactions with various N- and O-nucleophiles; therefore, they significantly extend the accessibility to the chemical space covered by organosulfur(VI) compounds with S=N bonds. In addition, previously unknown imidosulfuric diamides with free imino nitrogen groups were prepared, and their physical and chemical properties were characterized (including molecular geometry, pKa, Log P, microsomal stability, and reactivity towards typical electrophiles). Similar to other organosulfur(VI) derivatives with S=N bonds, these compounds can be considered as promising bioisosteres of amides, ureas, or sulfonamides. 相似文献