scholarly journals Synthesis, Characterization and Biological Evaluation of Metal(II) Complexes Containing Triphenylphosphine and Schiff Base Ligand Based on 3-Methoxysalicylaldehyde

2021 ◽  
Vol 33 (8) ◽  
pp. 1819-1823
Author(s):  
G. Gokulnath ◽  
P. Anitha ◽  
R. Manikandan ◽  
C. Umarani
Keyword(s):  
Schiff Base ◽  
Cancer Cell ◽  
Schiff Base Ligand ◽  
Cancer Cell Line ◽  
Biological Evaluation ◽  
Diffusion Method ◽  
Gram Positive Bacteria ◽  
Antimicrobial Efficiency ◽  
Nmr Techniques

Schiff base ligand (HL) derived from condensation of 3-methoxy salicylaldehyde with 4-aminobenzoic acid and its metal(II) complexes containing triphenylphosphine of the type [MCl(PPh3)(L)] (M = Ni2+, Co2+ or Cu2+; L = bitendate Schiff base ligand) have been synthesized. All the metal(II) complexes were characterized by analytical and spectroscopic (FT-IR, electronic, ESI-Mass, ESR, 1H, 13C NMR and 31P NMR) techniques. All the synthesized compounds were evaluated for in vitro antimicrobial efficiency against Gram-positive bacteria, Gram-negative bacteria and fungai using the agar well diffusion method. Anticancer activity in vitro of the ligand and its metal(II) complexes were also screened against MCF-7 cancer cell lines (human breast cancer cell line).

scholarly journals Novel Nonsymmetrically p-Benzyl-Substituted (Benz)imidazole N-Heterocyclic Carbene-Silver(I) Acetate Complexes: Synthesis and Biological Evaluation

2012 ◽  
Vol 2012 ◽  
pp. 1-13 ◽  
Author(s):  
Frauke Hackenberg ◽  
Anthony Deally ◽  
Grainne Lally ◽  
Sina Malenke ◽  
Helge Müller-Bunz ◽  
...  
Keyword(s):  
Cancer Cell Line ◽  
Benzyl Bromide ◽  
Biological Evaluation ◽  
Diffusion Method ◽  
X Ray Diffraction ◽  
Gram Positive Bacteria ◽  
Acetate Complex ◽  
Renal Cancer Cell ◽  
Synthesis And Biological Evaluation

Nonsymmetrically substituted N-heterocyclic carbene (NHC) precursors 1a–d and 3a–d were synthesised by first reacting 1H-(benz)imidazole with p-cyanobenzyl bromide to give 4-(1H-imidazole-1-ylmethyl)benzonitrile (1) and 4-(1H-benzimidazole-1-ylmethyl)benzonitrile (3) and afterwards introducing benzyl bromide, 1-(bromomethyl)-4-methylbenzene, 1-(bromomethyl)-4-methoxybenzene, and methyl 4-(bromomethyl)benzoate. The NHC-silver(I) acetate complexes (1-benzyl-3-(4-cyanobenzyl)-2,3-dihydro-1H-imidazole-2-ylidene) silver(I) acetate (2a), (1-(4-cyanobenzyl)-3-(4-methylbenzyl)-2,3-dihydro-1H-imidazole-2-ylidene) silver(I) acetate (2b), (1-(4-cyanobenzyl)-3-[4-(methoxycarbonyl)benzyl]-2,3-dihydro-1H-imidazole-2-ylidene) silver(I) acetate (2c), (1-benzyl-3-(4-cyanobenzyl)-2,3-dihydro-1H-benzimidazole-2-ylidene) silver(I) acetate (4a), (1-(4-cyanobenzyl)-3-(4-methylbenzyl)-2,3-dihydro-1H-benzimidazole-2-ylidene) silver(I) acetate (4b), (1-(4-cyanobenzyl)-3-(4-methoxybenzyl)-2,3-dihydro-1H-benzimidazole-2-ylidene) silver(I) acetate (4c), and (1-(4-cyanobenzyl)-3-[4-(methoxycarbonyl)benzyl]-2,3-dihydro-1H-benzimidazole-2-ylidene) silver(I) acetate (4d) were yielded by reacting these NHC precursors with silver(I) acetate. The silver(I) acetate complex 4b was characterised by single crystal X-ray diffraction. Preliminary in vitro antibacterial studies against the Gram-positive bacteria Staphylococcus aureus and the Gram-negative bacteria Escherichia coli, using the Kirby-Bauer disc diffusion method, were carried out on the seven NHC-silver(I) acetate complexes 2a–c and 4a–d. Also the IC50 values of these seven complexes were determined by an MTT-based assay against the human renal cancer cell line Caki-1. The complexes 2a–c and 4a–c revealed the following IC50 values, respectively, 25 (±1), 15 (±2), 5.4 (±0.8), 16 (±2), 7.1 (±1), 20 (±4), and 14 (±1) μM.

scholarly journals Antitumor and Antimicrobial Potential of Manganese(II), Nickel(II) and Copper(II) Complexes of 4-Methoxy Benzohydrazide Derived Schiff Base Ligand

2021 ◽  
Vol 11 (1) ◽  
pp. 3249-3260
Keyword(s):  
Schiff Base ◽  
Metal Complexes ◽  
Schiff Base Ligand ◽  
Antimicrobial Activities ◽  
Molar Ratio ◽  
Gram Positive Bacteria ◽  
Ft Ir ◽  
Dose Dependent

Herein, we describe the synthesis and characterization of a Schiff base ligand (E)-N'-(2-hydroxybenzylidene)-4-methoxybenzohydrazide (HBMB) and its Mn(II), Ni(II), and Cu(II) metal complexes (C1-C3) respectively. The ligand HBMB was synthesized by reacting condensation of salicylaldehyde and 4-methoxy benzohydrazide in a 1:1 molar ratio. The structure of HBMB and its metal complexes (C1-C3) were evaluated by using UV-Vis, FT-IR, 1H-NMR, mass spectroscopy as well as on the basis of elemental analysis, conductivity measurements, and thermogravimetric techniques (TGA). The synthesized molecules' tumoricidal properties were performed against human breast cancer (MCF-7) and colon cancer (HT 29) cell lines. The biological results indicated that the ligand, HBMB, and metal complexes possess dose-dependent selective cytotoxicity against the tested carcinoma cells. The synthesized compounds were further evaluated for their in vitro antimicrobial activities against Gram-positive bacteria (Staphylococcus aureus), Gram-negative bacteria (Escherichia coli), and fungal strains (Aspergillus niger).

scholarly journals Synthesis, Biological Evaluation and Docking Study of Etodolac-Triazole Conjugate

2020 ◽  
pp. 35-51
Author(s):  
Papigani Neeraja ◽  
Suryapeta Srinivas ◽  
Venkanna Banothu ◽  
Khagga Mukkanti ◽  
Pramod Kumar Dubey ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Triazole Ring ◽  
Docking Study ◽  
Biological Evaluation ◽  
Lung Cancer Cell Line ◽  
Human Lung Cancer ◽  
High Yield ◽  
Diffusion Method

A new set of 15 compounds containing etodolac moiety and triazole ring were prepared by CuAAC reaction in moderate to high yield. All the synthesized compounds were purified by chromatographic techniques and characterized by spectral data IR, 1H and 13C NMR and mass spectrometry. The newly derived compounds were screened for their anti-bacterial activities against one gram-positive (S. aureus) and two gram-negative (E. coli, K. pneumoniae) bacteria using an agar-well diffusion method. Most of the compounds showed good to moderate antibacterial activities. Especially compound 4e having good activities against all the strains. The compound 4e displayed significant inhibitory potential with MIC 25 µg/mL against all the strains. The potential DNA gyrase inhibitory activity of this compound was investigated by using molecular docking studies carried out using Autodock Vina software. The compound 4e showed the lowest ΔGbind results (-7.7 Kcal/mol, -7.9Kcal/mol). The cytotoxic activity of the obtained compounds was determined using A549 cancer cell line by a MTT assay. They displayed promising activity against the human lung cancer cell line. Especially 4o, 4b, 4d shown lowest IC50 values.

scholarly journals Synthesis, Characterization and Biological Evaluation of Schiff Base (N-4-(thiophene-2-yl-methyleneamino)-2,6-dimethylpyrimidine-4-yl)benzenesulfonamide and its Complexes with Cu(II), Ni(II), Co(II), Fe(II), Mn(II), Zn(II) Ions

2020 ◽  
Vol 71 (1) ◽  
pp. 206-212 ◽  
Author(s):  
Amina Mumtaz ◽  
Tariq Mahmud ◽  
M. R. J. Elsegood ◽  
G. W. Weaver ◽  
Gabriel Bratu ◽  
...  
Keyword(s):  
Schiff Base ◽  
Transition Metal ◽  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Schiff Base Ligand ◽  
Condensation Reaction ◽  
Klebsiella Oxytoca ◽  
Biological Evaluation ◽  
Anti Inflammatory

Two step synthesis of Schiff base ligand and its transition metal complexes was done by condensation reaction. In first step, the drug and aldehyde in equimolar ratio were refluxed for one hour at pH 8-9 in order to get Schiff base ligand. In second step, ligand and metal salts were refluxed for 2 hour. The ligand and Cu(II), Ni(II), Co(II), Fe(II), Mn(II), Zn(II) complexes were characterized by using different instruments like FT-IR, 1H-NMR, 13C-NMR, Mass, Atomic absorption spectrometer, Elemental analyzer, UV-visible spectrophotometer, Evans balance, Conductivitymeter and Thermogravimeter. In vitro antibacterial, antifungal and anti-inflammatory activities were also studied. The synthesized ligand and transition metal complexes were tested against Escherichia coli, Enterobacter aerogenes, Staphylococcus aureus, Bacillus pumilus, Klebsiella oxytoca, Clostridium butyrium, Mucor and Aspergillus niger. These studies demonstrated the enhanced activity of metal complexes against reported bacterial and fungal strains when compared with free Schiff base ligand. The Cu(II) complex recognized as anti-inflammatory agent while the parent drug showed no activity.

Synthesis, Design and Biological Evaluation of Antibacterial activity of novel mixed Metal Complexes derived from Benzoimidazolphenylethanamine and 6-Amino-N,N-dimethyluracil

2020 ◽  
Vol 17 ◽  
Author(s):  
Fahad M. Alminderej
Keyword(s):  
Metal Complexes ◽  
Micrococcus Luteus ◽  
Condensation Reaction ◽  
Antibacterial Activities ◽  
Biological Evaluation ◽  
Diffusion Method ◽  
Gram Positive Bacteria ◽  
Synthesis Design ◽  
Hybrid Complexes

: Benzoimidazolphenylethanamine (BPE) was synthesized through the condensation reaction of 1,2-phenyldiamine and L-phenylalanine. The new complexes were prepared from the reaction of 6-amino-N,N-dimethyluracil (ADU), benzoimidazolphenylethanamine and Cadmium (II), Tin (II), Copper (II) and Nickel (II) metal respectively. All new hybrid complexes were fully characterized by spectroscopic data of FTIR, UV-Visible electronic absorption, thermal analysis, X-ray powder diffraction studies and mass spectroscopy. Spectra analyses of the hybrid metal complexes showed the tetrahedral coordination of the ligands to the metal ions via the nitrogen atoms. The in vitro antibacterial activities of the hybrid complexes were assayed against four bacterial isolates namely, Micrococcus luteus, Staphylococcus aureus as gram positive bacteria, Pseudomonas aeruginosa and Escherichia coli as gram negative bacteria using agar well diffusion method. Most of the tested isolates were sensitive to most metal hybrid complexes. The drug likeness and bioactivity properties were calculated using Molinspiration Cheminformatics software.

Functionalized Nano-graphene Oxide as Multi-modal Clinic for Effective Drug Delivery

2017 ◽  
Vol 10 (4) ◽  
pp. 3768-3771
Author(s):  
Soumitra Satapathi ◽  
Rutusmita Mishra ◽  
Manisha Chatterjee ◽  
Partha Roy ◽  
Somesh Mohapatra
Keyword(s):  
Drug Delivery ◽  
Graphene Oxide ◽  
Cancer Cell ◽  
High Surface ◽  
High Surface Area ◽  
Cancer Cell Line ◽  
Xrd Analysis ◽  
Graphene Derivatives ◽  
Nano Graphene

Nano-materials based drug delivery modalities to specific organs and tissues has become one of the critical endeavors in pharmaceutical research. Recently, two-dimensional graphene has elicited considerable research interest because of its potential application in drug delivery systems. Here we report, the drug delivery applications of PEGylated nano-graphene oxide (nGO-PEG), complexed with a multiphoton active and anti-cancerous diarylheptanoid drug curcumin. Specifically, graphene-derivatives were used as nanovectors for the delivery of the hydrophobic anticancer drug curcumin due to its high surface area and easy surface functionalization. nGO was synthesized by modified Hummer’s method and confirmed by XRD analysis. The formation of nGO, nGO-PEG and nGO-PEG-Curcumin complex were monitored through UV-vis, IR spectroscopy. MTT assay and AO/EB staining found that nGO-PEG-Curcumin complex afforded highly potent cancer cell killing in vitro with a human breast cancer cell line MCF7.

Synthesis, Characterization and in vitro Biological Evaluation of a New Schiff Base Derived from Drug and its Complexes with Transition Metal Ions

2018 ◽  
Vol 69 (7) ◽  
pp. 1678-1681
Author(s):  
Amina Mumtaz ◽  
Tariq Mahmud ◽  
M. R. J. Elsegood ◽  
G. W. Weaver
Keyword(s):  
Schiff Base ◽  
Transition Metal ◽  
Metal Ions ◽  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Free Ligand ◽  
Transition Metal Ions ◽  
Biological Evaluation ◽  
Pyridoxal Hydrochloride

New series of copper (II), cobalt (II), zinc (II), nickel (II), manganese (II), iron (II) complexes of a novel Schiff base were prepared by the condensation of sulphadizine and pyridoxal hydrochloride. The ligand and metal complexes were characterized by utilizing different instrumental procedures like microanalysis, thermogravimetric examination and spectroscopy. The integrated ligand and transition metal complexes were screened against various bacteria and fungus. The studies demonstrated the enhanced activity of metal complexes against reported microbes when compared with free ligand.

New Platinum (II) Ternary Complexes of Formamidine and Pyrophosphate: Synthesis, Characterization and DFT Calculations and In vitro Cytotoxicity

2020 ◽  
Vol 23 (7) ◽  
pp. 611-623
Author(s):  
Ahmed A. Soliman ◽  
Fawzy A. Attaby ◽  
Othman I. Alajrawy ◽  
Azza A.A. Abou-hussein ◽  
Wolfgang Linert
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Theoretical Calculations ◽  
Thermal Analyses ◽  
Cancer Cell Line ◽  
Cellular Growth ◽  
Planar Geometry ◽  
Square Planar ◽  
Vis Spectroscopy

Aim and Objective: Platinum (II) and platinum (IV) of pyrophosphate complexes have been prepared and characterized to discover their potential as antitumor drugs. This study was conducted to prepare and characterize new ternary platinum (II) complexes with formamidine and pyrophosphate as an antitumor candidate. Materials and Methods: The complexes have been characterized by mass, infrared, UV-Vis. spectroscopy, elemental analysis, magnetic susceptibility, thermal analyses, and theoretical calculations. They have been tested for their cytotoxicity, which was carried out using the fastcolorimetric assay for cellular growth and survival against MCF-7 (breast cancer cell line), HCT- 116 (colon carcinoma cell line), and HepG-2 (hepatocellular cancer cell line). Results: All complexes are diamagnetic, and the electronic spectral data displayed the bands due to square planar Pt(II) complexes. The optimized complexes structures (1-4) indicated a distorted square planar geometry where O-Pt-O and N-Pt-N bond angles were 82.04°-96.44°, respectively. Conclusion: The complexes showed noticeable cytotoxicity and are considered as promising antitumor candidates for further applications.

A Novel Triazole Derivative Drug Presenting In Vitro and In Vivo Anticancer Properties

2018 ◽  
Vol 18 (17) ◽  
pp. 1483-1493
Author(s):  
Ricardo Imbroisi Filho ◽  
Daniel T.G. Gonzaga ◽  
Thainá M. Demaria ◽  
João G.B. Leandro ◽  
Dora C.S. Costa ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Hepatic Function ◽  
Anticancer Properties ◽  
Mcf 7

Background: Cancer is a major cause of death worldwide, despite many different drugs available to treat the disease. This high mortality rate is largely due to the complexity of the disease, which results from several genetic and epigenetic changes. Therefore, researchers are constantly searching for novel drugs that can target different and multiple aspects of cancer. Experimental: After a screening, we selected one novel molecule, out of ninety-four triazole derivatives, that strongly affects the viability and proliferation of the human breast cancer cell line MCF-7, with minimal effects on non-cancer cells. The drug, named DAN94, induced a dose-dependent decrease in MCF-7 cells viability, with an IC50 of 3.2 ± 0.2 µM. Additionally, DAN94 interfered with mitochondria metabolism promoting reactive oxygen species production, triggering apoptosis and arresting the cancer cells on G1/G0 phase of cell cycle, inhibiting cell proliferation. These effects are not observed when the drug was tested in the non-cancer cell line MCF10A. Using a mouse model with xenograft tumor implants, the drug preventing tumor growth presented no toxicity for the animal and without altering biochemical markers of hepatic function. Results and Conclusion: The novel drug DAN94 is selective for cancer cells, targeting the mitochondrial metabolism, which culminates in the cancer cell death. In the end, DAN94 has been shown to be a promising drug for controlling breast cancer with minimal undesirable effects.

Synthesis, Docking Study, Cytotoxicity, Antioxidant, and Anti-microbial Activities of Novel 2,4-Disubstituted Thiazoles Based on Phenothiazine

2020 ◽  
Vol 17 (2) ◽  
pp. 151-159
Author(s):  
Tran Nguyen Minh An ◽  
Pham Thai Phuong ◽  
Nguyen Minh Quang ◽  
Nguyen Van Son ◽  
Nguyen Van Cuong ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Antimicrobial Activities ◽  
Significant Activity ◽  
Thiazole Derivatives ◽  
Ligand Interaction ◽  
Ic50 Value ◽  
Mcf 7

: A series of novel 1,3-thiazole derivatives (5a-i) with a modified phenothiazine moiety were synthesized and tested against cancer cell line MCF-7 for their cytotoxicity. Most of them (5a-i) were less cytotoxic or had no activity against MCF-7 cancer cell line. Material and Methods: The IC50 value of compound (4) was 33.84 μM. The compounds (5a-i) were also evaluated for antimicrobial activities, but no significant activity was observed. The antioxidant activity was conducted for target compounds (5a-i). The IC50 value of compound (5b) was 0.151mM. Results: The total amount of energy, ACE (atomic contact energy), energy of receptor (PDB: 5G5J), and ligand interaction of structure (4) were found to be 22.448 Kcal.mol-1 , -247.68, and -91.91 Kcal.mol-1, respectively. The structure (4) is well binded with the receptor because the values of binding energy, steric energy, and the number of hydrogen bondings are -91.91, 22.448 kcal.mol-1, and 2, respectively. It shows that structure (4) has good cytotoxicity with MCF-7 in vitro. Conclusion: The increasing of docking ability of structures (5a-i) with the receptor is presented in increasing order as (5f)>(5e)>(5g)>(5a)>(5b)>(5d)>(5c)>(5i)>(5h). The structure bearing substitution as thiosemicarbazone (4), nitrogen heterocyclic (5f), halogen (5e), and azide (5g) showed good cytotoxicity activity in vitro.

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