832-89-3Relevant articles and documents
Polyamine ligand-mediated self-assembly of gold and silver nanoparticles into chainlike structures in aqueous solution: Towards new nanostructured chemosensors
Fernandez-Lodeiro, Adrian,Fernandez-Lodeiro, Javier,Nunez, Cristina,Bastida, Rufina,Capelo, Jose Luis,Lodeiro, Carlos
, p. 200 - 207 (2013)
1D Nanochain formation: The binding ability of a polyamine molecular linker (L)2- bearing different functional groups, which favors the self-assembling of silver (AgNPs) and gold nano-particles (AuNPs) into 1D nanochains in aqueous solution was explored. UV/Vis spectrophotometry and TEM were used to determine time-dependent structural changes associated with these 1D structure formations. Sensing of Hg2+ using AgNPs@ (L) 2- and AuNPs@ (L)2- assemblies was also carried out in aqueous solution.
Luminescent sensing of dicarboxylates in water by a bismacrocyclic dinuclear Eu(III) conjugate
Plush, Sally E.,Gunnlaugsson, Thorfinnur
, p. 1919 - 1922 (2007)
The design, synthesis, and characterization of a novel dinuclear Eu(III) bismacrocyclic conjugate 1·Eu2 as a delayed luminescent lanthanide sensor for dicarboxylates is discussed. The sensor was shown to bind small dicarboxylic acids such as aspartic, malonic, succinic, or glutaric acid in pH 6.5 solutions. However, only malonic acid gave rise to selective Eu(III) luminescent enhancements, as the emission was reduced for all of the other acids.
Naphthalene appended 2,5-diketopiperazine towards fluorometric response of dihydrogenphosphate
Ghosh, Kumaresh,Sen, Tanushree
, p. 447 - 452 (2010)
Naphthalene-based 2,5-diketopiperazine 1 has been synthesized in two steps with moderate yield. The compound shows water templated hydrogen bonded assemblies in the solid state and exhibits unique hydrogen bond mediated emission properties in solution. The monomer emission of 1 in CHCl3 containing 0.1% DMSO is significantly quenched in the presence of large excess of dihydrogenphosphate anion and aliphatic dicarboxylic acids of different chain lengths followed by the appearance of a new peak of moderate intensity at higher wavelength for excimer. The appearance of excimer emission of moderate intensity in presence of H2PO4- distinguishes it from other guests in the present study.
Unravelling the anticancer potency of 1,2,4-triazole-N-arylamide hybrids through inhibition of STAT3: synthesis and in silico mechanistic studies
Turky, Abdallah,Bayoumi, Ashraf H.,Sherbiny, Farag F.,El-Adl, Khaled,Abulkhair, Hamada S.
, p. 403 - 420 (2020/08/25)
Abstract: The discovery of potent STAT3 inhibitors has gained noteworthy impetus in the last decade. In line with this trend, considering the proven biological importance of 1,2,4-triazoles, herein, we are reporting the design, synthesis, pharmacokinetic profiles, and in vitro anticancer activity of novel C3-linked 1,2,4-triazole-N-arylamide hybrids and their in silico proposed mechanism of action via inhibition of STAT3. The 1,2,4-triazole scaffold was selected as a privilege ring system that is embedded in core structures of a variety of anticancer drugs which are either in clinical use or still under clinical trials. The designed 1,2,4-triazole derivatives were synthesized by linking the triazole-thione moiety through amide hydrophilic linkers with diverse lipophilic fragments. In silico study to predict cytotoxicity of the new hybrids against different kinds of human cancer cell lines as well as the non-tumor cells was conducted. The multidrug-resistant human breast adenocarcinoma cells (MDA-MB-231) was found most susceptible to the cytotoxic effect of synthesized compounds and hence were selected to evaluate the in vitro anticancer activity. Four of the designed derivatives showed promising cytotoxicity effects against selected cancer cells, among which compound 12 showed the highest potency (IC50 = 3.61?μM), followed by 21 which displayed IC50 value of 3.93?μM. Also, compounds 14 and 23 revealed equipotent activity with the reference cytotoxic agent doxorubicin. To reinforce these observations, the obtained data of in vitro cytotoxicity have been validated in terms of ligand–protein interaction and new compounds were analyzed for ADMET properties to evaluate their potential to build up as good drug candidates. This study led us to identify two novel C3-linked 1,2,4-triazole-N-arylamide hybrids of interesting antiproliferative potentials as probable lead inhibitors of STAT3 with promising pharmacokinetic profiles. Graphic abstract: [Figure not available: see fulltext.]
Novel selective ido1 inhibitors with isoxazolo[5,4-d]pyrimidin-4(5h)-one scaffold
?vajger, Urban,Bratkovi?, Toma?,Dol?ak, Ana,Gobec, Stanislav,Mlinari?, Larisa,Ogorevc, Eva,Sova, Matej
, (2021/04/02)
Indoleamine 2,3-dioxygenase 1 (IDO1) is a promising target in immunomodulation of several pathological conditions, especially cancers. Here we present the synthesis of a series of IDO1 inhibitors with the novel isoxazolo[5,4-d]pyrimidin-4(5H)-one scaffold. A focused library was prepared using a 6-or 7-step synthetic procedure to allow a systematic investigation of the structure-activity relationships of the described scaffold. Chemistry-driven modifications lead us to the discovery of our best-in-class inhibitors possessing p-trifluoromethyl (23), p-cyclohexyl (32), or p-methoxycarbonyl (20, 39) substituted aniline moieties with IC50 values in the low micromolar range. In addition to hIDO1, compounds were tested for their inhibition of indoleamine 2,3-dioxygenase 2 and tryptophan dioxygenase, and found to be selective for hIDO1. Our results thus demon-strate a successful study on IDO1-selective isoxazolo[5,4-d]pyrimidin-4(5H)-one inhibitors, defining promising chemical probes with a novel scaffold for further development of potent small-molecule immunomodulators.
Synthesis of New Thieno[2,3-d]pyrimidines Containing a 1,2,3-Triazole Ring and Their Therapeutic Response in NCI-60 Cell Line Panel
Baluja, S. H.,Bhensdadia, K. A.,Lalavani, N. H.
, p. 1668 - 1677 (2021/12/13)
Abstract: A series of new tetrahydro[1]benzothieno[2,3-d]pyrimidines containing a 1,2,3-triazole fragment linkedthrough an oxymethylene spacer have been synthesized by click reaction of4-(prop-2-yn-1-yloxy)-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidines with various aryl and alkyl azides inthe presence of copper sulfate and sodium ascorbate as a catalyst. Thestructures of the synthesized compounds were characterized by variousspectroscopic techniques (1H and13C NMR, FT-IR, and mass spectrometry), and theirin vitro anticancer activity against NCI-60 human tumor cell lines wasevaluated. Among the compounds tested, N-(pyridine-3-yl)-acetamide derivative exhibited significantactivity against several cancer cell lines, including SF-539 (CNS cancer),HCT-116 (colon cancer), OVCAR-8 (ovarian cancer), PC-3 (prostate cancer), andCCRF-CEM (leukemia).
