51236-93-2Relevant academic research and scientific papers
Modifying aroylhydrazone prochelators for hydrolytic stability and improved cytoprotection against oxidative stress
Wang, Qin,Franz, Katherine J.
, p. 5962 - 5972 (2018)
BSIH ((E)-N′-(2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzylidene)isonicotinohydrazide) is a prodrug version of the metal chelator SIH ((E)-N′-(2-hydroxybenzylidene)isonicotinohydrazide) in which a boronate group prevents metal chelation until reac
Mixed-ligand metal complexes containing an ONS Schiff base and imidazole/benzimidazole ligands: Synthesis, characterization, crystallography and biological activity
Mazlan, Nurul Ain,Ravoof, Thahira Begum S. A.,Tiekink, Edward R. T.,Tahir, Mohamed Ibrahim Mohamed,Veerakumarasivam, Abhi,Crouse, Karen A.
, p. 633 - 639 (2014)
Salicylaldehyde-4-methylthiosemicarbazone (H2MTSali) has been prepared via the condensation reaction of 4-methyl-3-thiosemicarbazide and salicylaldehyde. Four new mixed-ligand copper(II) and nickel(II) complexes with a general formula [M(MTSali)L] (M = Cu2+ or Ni2+; L = co-ligand) were synthesized, where L is either imidazole (im) or benzimidazole (bzim). The Schiff base and its mixed-ligand complexes were characterized by IR and UV/Vis spectroscopy, and the complexes by molar conductivity and magnetic susceptibility measurements. The spectroscopic data indicated that the Schiff base behaves as a tridentate ONS donor ligand coordinating via the phenoxide-oxygen, azomethine-nitrogen, and thiolate-sulphur atoms. Magnetic data indicate a square planar environment for the nickel(II) complexes while molar conductance values indicate that the metal complexes are essentially non-electrolytes in DMSO solution. X-ray crystallography shows Cu(MTSali)bzim (1) and Ni(MTSali)bzim (3) to be isostructural, with the metal(II) ions being coordinated by a N2OS donor set that defines an approximate square planar geometry; in both cases, the benzimidazole is splayed with respect to the coordination plane. The copper(II) complexes were active against MDA-MB-231 and MCF-7 breast cancer cell lines, more so than H2MTSali, whereas the nickel(II) complexes were inactive.
Four copper(II) compounds synthesized by anion regulation: Structure, anticancer function and anticancer mechanism
Zhang, Zhenlei,Gou, Yi,Wang, Jun,Yang, Kun,Qi, Jinxu,Zhou, Zuping,Liang, Shichu,Liang, Hong,Yang, Feng
, p. 399 - 409 (2016)
Copper (Cu) compounds are a promising candidate for next generation metal anticancer drugs. Therefore, we regulated anions to synthesize four mononuclear and binuclear Cu(II) compounds derived from thiosemicarbazone Schiff base ligands and characterized them. Four of these compounds showed very high cytotoxicity to cancer cell lines in vitro. These Cu(II) compounds strongly promoted the apoptosis of BEL-7404 cells and had a capacity to arrest the cell cycle at S phase of those cells. Furthermore, reactive oxygen species (ROS), mitochondrial membrane potential and Western blot analyses revealed that these Cu(II) compounds exert their cytotoxicity through an ROS-mediated intrinsic mitochondrial pathway accompanied by the regulation of Bcl-2 family proteins.
Structures and antimicrobial activity of fluoro- and hydroxy-substituted thiocarboxyhydrazones
Liu
, p. 1420 - 1425 (2015)
A series of fluoro- and hydroxy-substituted thiocarboxyhydrazones, 2-(3-fluorobenzylidene)-Nmethylhydrazinecarbothioamide (1), 2-(2,3-difluorobenzylidene)-N-methylhydrazinecarbothioamide (2), and 2-(2-hydroxybenzylidene)-N-methylhydrazinecarbothioamide (3
ROLES OF MODULATORS OF INTERSECTIN-CDC42 SIGNALING IN ALZHEIMER'S DISEASE
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Paragraph 0283; 0285; 0289, (2019/04/14)
Methods of treating Alzheimer's disease and other neurodegenerative and/or neurocognitive and/or neurodevelopmental diseases are described. The methods comprise the administration of compounds that modulate an activity of cell division control protein 42 (Cdc42), such as the interaction between Cdc42 and intersectin (ITSN). Exemplary modulator compounds include thioureas, disulfonamides of fused aromatic systems (e.g., benzofuran), and acyl hydrazones, among others. Some of the modulator compounds act as activators of Cdc42, while others act as inhibitors. In some cases, the modulator compound has dual functionality and the ability of the modulator compound to act as an inhibitor or activator depends on whether or not Cdc42 is already activated in a particular disease stage or biological environment by an upstream activating signal of Cdc42.
In-house chemical library repurposing: A case example for Pseudomonas aeruginosa antibiofilm activity and quorum sensing inhibition
Ravithej Singh,Tripathi, Vikash C.,Raj, Sneha,Kumar, Anoop,Gupta, Sampa,Horam, Soyar,Upadhyay, Akanksha,Kushwaha, Pragati,Arockiaraj, Jesu,Sashidhara, Koneni V.,Pasupuleti, Mukesh
, p. 383 - 390 (2018/10/15)
(Table presented.). Drug repurposing has become a recent trend in drug development programs, where previously developed drugs are explored for hit and redeveloped into potential therapeutic agents for new diseases. Globally, in any drug development progra
Synthesis, spectroscopic and crystallographic characterization of the cobalt(III) ternary mixed-ligand complexes of N(4)-allyl/methyl thiosemicarbazones, N,N,Nae,Nae-tetramethylethylenediamine and azide
Bal-Demirci, Tuelay,Akkurt, Mehmet,YalcIn, Serife Pinar,Bueyuekguengoer, Orhan
experimental part, p. 95 - 102 (2011/12/15)
Mixed-ligand ternary cobalt(III) complexes consisting of N,N,Nae,Nae-tetramethylethylenediamine (tmen), R-salicylaldehyde-N(4)-allyl/methyl thiosemicarbazones (R=3-OMe (LI/LII) or H (LIII/LIV) and azide, of general formula [CoL(tmen)(N3)], were synthesized and characterized by physico-chemical and spectroscopic methods. The crystal structure of [CoLI(tmen)(N3)] has a slightly distorted octahedral coordination geometry involving the O, N and S atoms of thiosemicarbazone.
Novel synthesis of new 5,7-disubstituted-2-alkyl/arylamino-4H-pyrazolothiadiazines and 4,6-disubstituted-3-amino/anilino-2-alkyl/aryliminopyrazolothiazolines
Chande, Madhukar S.,Joshi, Rajesh D.
, p. 289 - 301 (2007/10/02)
The title compounds have been prepared by the interaction of substituted 4-bromopyrazolin-5-ones with thiosemicarbazides.An alternate unambiguous synthesis of pyrazolothiazolines has been described.All the compounds have been characterised by spect
