scholarly journals Synthesis, Structure, Electrochemistry, and Spectral Characterization of Bis-Isatin Thiocarbohydrazone Metal Complexes and Their Antitumor Activity Against Ehrlich Ascites Carcinoma in Swiss Albino Mice

2008 ◽  
Vol 2008 ◽  
pp. 1-11 ◽  
Author(s):  
M. P. Sathisha ◽  
V. K. Revankar ◽  
K. S. R. Pai

The synthesis, structure, electrochemistry, and biological studies of Co(II), Ni(II), Cu(II), and Zn(II) complexes of thiocarbohydrazone ligand are described. The ligand is synthesized starting from thiocarbohydrazide and isatin. It is evident from the IR data that in all the complexes, only one part of the ligand is coordinated to the metal ion resulting mononuclear complexes. The ligand coordinates essentially through the carbonyl oxygen of the isatin fragment, the nitrogen atom of the azomethine group, and sulfur atom after deprotonation to give five membered rings. H1 NMR spectrum of the ligand shows only one set of signals for the aromatic protons, while the NH of isatin and NH of hydrazone give rise to two different singlets in the 11–14 ppm range. The formulations, [Cu(L)Cl]·2H2O, [Cu(L)(CH3COO)]·2H2O, [Ni(L)Cl], [Ni(L)(CH3COO)], [Co(L2)], and [Zn(L2)]·2H2O are in accordance with elemental analyses, physical, and spectroscopic measurements. The complexes are soluble in organic solvents. Molar conductance values in DMF indicate the nonelectrolytic nature of the complexes. Copper complex displays quasireversible cyclic voltametric responses with Ep near −0.659 v and 0.504 v Vs Ag/AgCl at the scan rate of 0.1 V/s. Copper(II) complexes show a single line EPR signals. For the observed magnetic moment and electronic spectral data possible explanation has been discussed. From all the available data, the probable structures for the complexes have been proposed. The compounds synthesized in present study have shown promising cytotoxic activity when screened using the in vitro method and at the same time were shown to have good activity when tested using the Ehrlich ascites carcinoma (EAC) model. The antimicrobial screening showed that the cobalt complex possesses enhanced antimicrobial activity towards fungi.

MedChemComm ◽  
2017 ◽  
Vol 8 (5) ◽  
pp. 1103-1111 ◽  
Author(s):  
Entsar A. Saad ◽  
Mohamed M. Hassanien ◽  
Hatem A. El-mezayen ◽  
Nada M. ELmenawy

Cisplatin as a chief chemotherapy has nephro-toxicity and so we have tried to develop a novel antitumor drug based on a combination of cobalt metal ion with an organic moiety.


2020 ◽  
Vol 15 (2) ◽  
pp. 61-72

New pyrazine carbohydra zone ligand N'-(1-(5-chloro-2-hydroxyphenyl) ethylidene) pyrazine-2-carbohydrazide (H2L), prepared by the condensation of equimolar amounts of pyrazine-2-carbohydrazide with 2-hydroxy-5-chloroacetophenone in methanol, reacts with suitable metal salt precursors to give complexes of two general formulae: [M(HL)(Cl)(H2O)2] {M = Mn(II), Co(II), Ni(II) and Cu(II)} and [M(L)(H2O)] {M = Zn(II) and Cd(II)}. Structure of ligand was confirmed by elemental analysis, IR, 1H and 13C NMR and mass spectroscopy, while synthesized complexes were additionally characterized by magnetic susceptibility measurements, molar conductivity measurements, XRD, ESR (for Cu(II)), SEM and thermogravimetric analysis. Spectroscopic studies confirmed a tridentate ONO donor behavior of the ligand towards the central metal ion. The molar conductance (12–17 W–1 cm2 mol–1) measurements in DMSO indicated non-electrolytic nature. Thermal behavior of the complexes suggests their extended stability and the thermal decomposition generally proceeds via partial loss of the organic moiety and ends with the formation of respective metal oxide as a final product. Various kinetic and thermodynamic parameters were evaluated using the Coats-Redfern method. The solid-state electrical conductivity of the complexes measured in the temperature range 303-463 K suggested their semiconducting behavior. The ligand and its metal complexes were screened in vitro for their antibacterial activity against the Gram-positive bacteria S. aureus and B. subtilis, the Gram-negative bacteria E. coli and S. typhi and the fungi C. albicans and A. niger. The obtained results indicated improved activity of the complexes compared to the free ligand against all studied bacterial and fungal species.


2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Ikechukwu P. Ejidike ◽  
Peter A. Ajibade

Co(II), Ni(II), Cu(II), and Zn(II) complexes of (4E)-4-[(2-{(E)-[1-(2,4-dihydroxyphenyl)ethylidene]amino}ethyl)imino]pentan-2-one have been synthesized and characterized by elemental analyses, molar conductance, electronic and IR spectral studies, and XRD. FTIR confirmed the ligand coordinates the metal ion to form mononuclear complex via the oxygen and nitrogen atoms of the phenolic group and azomethine group, respectively. Tetrahedral geometry is proposed for Co(II) complex and square-planar geometry for Ni(II) and Cu(II) complexes. The antibacterial studies of the compounds were determined and they show that the metal complexes are more active than the free ligands. The antioxidant activity by DPPH and ABTS method was examined and it shows Cu(II); IC50= 2.31 ± 1.54 µM for DPPH and Co(II); IC50= 1.83 ± 1.08 µM for ABTS were the most active.


1970 ◽  
Vol 48 (4) ◽  
pp. 517-519 ◽  
Author(s):  
I. C. Caldwell ◽  
Marianne F. Chan

A number of incubation media which have been used in studies of the metabolism of Ehrlich ascites carcinoma (EAC) cells in vitro have been examined with respect to their abilities to support the incorporation of radioactive precursors into nucleotides and nucleic acids, and to maintain the structural integrity and tumor-inducing abilities of EAC cells. Cells incubated in the chemically-defined "Fischer's medium for leukemic cells of mice" were able to produce lethal tumors in mice after more than 16 h of incubation, maintained their structural integrity on prolonged incubation, and catalyzed high rates of incorporation of exogenously added substrates into nucleotides, RNA, and DNA. However, cells incubated in balanced salts solutions supplemented with glucose had these characteristics: (a) were unable to produce lethal tumors after 4 h of incubation, (b) released large amounts of nucleotide, nucleic acid, and protein material into the medium after less than 2 h of incubation, and (c) catalyzed the incorporation of radioactive precursors into nucleotides and RNA at much lower rates than did cells incubated in Fischer's medium, and were virtually unable to catalyze the incorporation of adenine-14C into DNA.


1965 ◽  
Vol 43 (2) ◽  
pp. 209-224 ◽  
Author(s):  
B. I. Uppin ◽  
P. G. Scholefield

Studies have been made of the effects of metabolic inhibitors on the oxidation and incorporation of radioactivity into nucleotides of glucose labelled in the 1, 2, and 6 positions. The results indicate that in Ehrlich ascites carcinoma cells the predominant oxidative pathway is the hexosemonophosphate shunt. Investigation of the time courses of oxidation of the labelled glucose molecules confirms this conclusion. The pattern of incorporation of radioactivity initially suggests that nucleotide ribose is not formed via this pathway. However, it is shown that the coupling of an active transketolase system with the other enzymes of the hexosemonophosphate shunt provides a sufficient explanation of all the experimental observations. The conclusion is reached that pentose is formed by oxidation of glucose through the shunt but that the labelling pattern is largely established as the result of the exchange reaction catalyzed by transketolase.


2012 ◽  
Vol 9 (3) ◽  
pp. 532-540 ◽  
Author(s):  
Baghdad Science Journal

Two Schiff base ligands L1 and L2 have been obtained by condensation of salicylaldehyde respectively with leucylalanine and glycylglycine then their complexes with Zn(II)were prepared and characterized by elemental analyses , conductivity measurement , IR and UV-Vis .The molar conductance measurement indicated that the Zn(II) complexes are 1:1 non-electrolytes. The IR data demonstrated that the tetradentate binding of the ligands L1 and L2 . The in vitro biological screening effect of the investigated compounds have been tested against the bacterial species Staphlococcus aureus, Escherichia coil , Klebsiella pneumaniae, Proteus vulgaris and Pseudomonas aeruginosa by the disc diffusion method . A comparative study of inhibition values of the Schiff base ligands and their complexes indicated that the complexes exhibit higher antimicrobial activity than the free ligands . Zinc ions are proven to be essential for the growth-inhibitor effect. The extent of inhibition appeared to be strongly dependent on the initial cell density and on the growth medium .


2021 ◽  
Vol 5 (3) ◽  
pp. 033-037
Author(s):  
Uma Nath U ◽  
Ravi. R ◽  
Sundara Ganapathy ◽  
Lal Prasanth

This study was designed to determine the in vitro anticancer potential of the Astaxanthin isolated from shrimp shell waste (ETC) against Ehrlich Ascites Carcinoma (EAC) induced cancer in swiss albino mice. The anticancer activity was assessed using in vitro cytotoxicAity, mean survival time, tumor volume and hematological studies. The reliable criteria for evaluating the potential of any anticancer agent is the prolongation of lifespan of the animal and decrease in WBC count of blood. The high dose of ETC (200 mg/kg, orally) significantly reduced the tumor growth which was demonstrated by increased lifespan of the mice and restoration of hematological parameters. ETC was also found to be cytotoxic in the in vitro parameter which shows that ETC possesses significant anticancer potential.


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