15191-68-1Relevant articles and documents
Synthesis, characterization and cell viability test of six vanadyl complexes with acetylacetonate derivatives
Sgarbossa, Speranza,Diana, Eliano,Marabello, Domenica,Deagostino, Annamaria,Cadamuro, Silvano,Barge, Alessandro,Laurenti, Enzo,Gallicchio, Margherita,Boscaro, Valentina,Ghibaudi, Elena
, p. 26 - 37 (2013)
Vanadium compounds are known to display a number of therapeutic effects, namely insulin-mimetic and cardiovascular effects. Evidence of the antiproliferative and proapoptotic activity of a number of vanadyl complexes, together with their low toxicity, establishes these metal compounds as promising antitumoral therapeutic agents. In the present work, we describe the synthesis and full characterization of six new vanadyl complexes with acetylacetonate derivatives bearing asymmetric substitutions on the β-dicarbonyl moiety: the complexes were characterized in the solid state as well as in solution. Our results show that all complexes are in square pyramidal geometry; cis isomers in the equatorial plane are favored in the presence of strongly coordinating solvents. EPR evidence suggests that all complexes are in the bis-chelate form, although in two cases the mono-chelated complex seems to be present as well. Preliminary tests carried out on non-tumor and tumor cell lines show that these complexes are effective in suppressing cell viability and elicit a distinct response of tumor and non-tumor cells.
Synthesis and photoluminescent properties of Eu (III) complexes with fluorinated β-diketone and nitrogen heterocyclic ligands
Wang, Dan,Luo, Zheng,Liu, Zhao,Wang, Dunjia,Fan, Ling,Yin, Guodong
, p. 398 - 404 (2016)
Two fluorinated β-diketones and their six europium (III) complexes using 2,2-dipyridine, 1,10-phenanthroline or 4′-phenyl-terpyridine as the secondary ligand were synthesized and characterized. The photoluminescence behavior for these complexes was investigated in solid state in detail. Based on the emission spectra and luminescence decay curves of these complexes in solid state, the Judd-Ofelt intensity parameters (Ωt), lifetime (τ) and luminescence quantum efficiency (η) were determined. The Ω2 values indicate that the europium (III) ion is in a highly polarizable chemical environment in these complexes. Europium (III) complexes with the secondary ligands 2,2-dipyridine or 1,10-phenanthroline exhibited much better photoluminescence properties than complexes with the secondary ligand 4′-phenyl-terpyridine. Especially, europium (III) complexes of 4,4,4-trifluoro-1-(4-fluorophenyl)-butane-1,3-dione containing the secondary ligands 2,2-dipyridine or 1,10-phenanthroline showed a longer lifetime (τ = 0.799 and 0.826 ms, respectively) and a higher luminescence quantum efficiency (η = 56.5 and 56.1, respectively) among these complexes.
Fay et al.
, p. 7056 (1970)
An Integrated Continuous Flow Micro-Total Ultrafast Process System (μ-TUFPS) for the Synthesis of Celecoxib and Other Cyclooxygenase Inhibitors
Sthalam, Vinay Kumar,Singh, Ajay K.,Pabbaraja, Srihari
supporting information, p. 1892 - 1899 (2019/10/11)
Integrated continuous manufacturing has emerged as a promising device for the rapid manufacturing of active pharmaceutical ingredients (APIs). We herein report a newly designed continuous flow micro-total process system platform for the rapid manufacturing of celecoxib, a selective nonsteroidal anti-inflammatory drug. This approach has been proven generally for the synthesis of several alkyl and aryl substituted pyrazoles. In order to minimize the tedious work-up process of potential reaction intermediates/products, we have developed a continuous flow extraction and separation platform to carry out the entire reaction sequence resulting in a short residence time with good yield. The present process was further extended to gram-scale synthesis of the COX-2-related API, viz. celecoxib, in the continuous flow process.
Design and synthesis of novel benzenesulfonamide containing 1,2,3-triazoles as potent human carbonic anhydrase isoforms I, II, IV and IX inhibitors
Kumar, Rajiv,Vats, Lalit,Bua, Silvia,Supuran, Claudiu T.,Sharma, Pawan K.
, p. 545 - 551 (2018/06/18)
In a quest to discover new biologically active compounds, a series of twenty novel heterocyclic derivatives substituted at position 5 with -H (7a-7j) or -CF3 (8a-8j), bearing benzenesulfonamide at N-1 position and various aroyl groups at position 4 of the 1,2,3-triazole ring was synthesized and screened for their carbonic anhydrase (CA, EC 4.2.1.1) inhibition potential against four human (h) isoforms hCA I, II, IV and IX. All the compounds (7a-7j and 8a-8j) were synthesized via [3+2] cycloaddition reaction from 4-azidobenzenesulfonamide. Interestingly, compounds 7a-7j were prepared in one pot manner via enaminone intermediate using novel methodology. All the newly synthesized compounds (7a-7j & 8a-8j) were found to be excellent inhibitors of edema related isoform hCA I with their inhibition constant (Ki) ranging from 30.1 to 86.8 nM as compared to standard drug acetazolamide (AAZ) with Ki = 250 nM. Further it was found that most of tested compounds were weaker inhibitors of isoform, hCA II although compounds 7b, 7d-7e, 8a, 8d-8f, 8i (mostly with electron withdrawing substituents) have shown better inhibition potential (Ki i = 52.4 nM) than AAZ (Ki = 74 nM) while against tumor associated hCA IX, all the compounds have shown moderate inhibition potential. Present study have added one more step in exploring the 1,2,3-triazlole moiety in the medicinal field.
