scholarly journals Synthesis, characterization, antimicrobial screening and cytotoxic properties of Cu(II) and Zn(II) complexes with bidentate hydroxylated 1,3-diaryl-2-propene-1-ones ligand

2020 ◽  
pp. 68-68
Author(s):  
Pravinkumar Patil ◽  
Sainath Zangade
Keyword(s):  
Antimicrobial Activity ◽  
Metal Complexes ◽  
Cytotoxic Activity ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Artemia Salina ◽  
Carbonyl Oxygen ◽  
Planar Geometry ◽  
Ft Ir

A series of binary metal complexes [halo, hydroxyl and methoxy sub-stituted bis (2-(E) acryloyl)naphthalen-1-yl)oxy)Cu(II) and Zn(II) (C1-C10)] of Cu2+ and Zn2+ ions derived from bi-coordinated hydroxylated 1,3-diaryl-2- -propene-1-ones were synthesized. The newly synthesized metal complexes were structurally determined by FT-IR, 1H NMR, 13CNMR, ESR spectral, XRD and TGA analysis. The FT-IR and ESR studies demonstrated that interactions between metal ions with ligands occur through carbonyl oxygen and deprotonated hydroxyl oxygen and corresponds to square-planar geometry for all complexes. In-vitro the metal complexes were screened and evaluated for their antimicrobial and cytotoxic activity. The complexes C1 and C4 showed the significant antimicrobial activity while the remaining complexes were showed the moderately antimicrobial activity against the tested pathogens. The complexes were evaluated for cytotoxic activity against the organism Artemia salina. The complexes C2, C3, C4 and C5 were showed the LC50 values as 630.45, 969.99, 921.94 and 918.41 ?M mL-1 respectively. Further complexes were evaluated for anticancer activity against liver cancer cell line (Hep G2) in comparison with 5-fluorouracil standard. The complex C5 showed the significant IC50 value 58.94 ?g mL-1. Therefore the present study is useful to develop the new class of antimicrobial and anticancer agents.

scholarly journals Synthesis, Characterisation, Antimicrobial activity and DNA Cleavage of (E)-2-((Tetrazolo[1,5-A]Quinolin-4- ylmethylene)Amino)Phenol Schiff base Metal complexes

2020 ◽  
Vol 13 (2) ◽  
pp. 29-37
Author(s):  
Anilkumar Ambala ◽  
Ch. Abraham Lincoln
Keyword(s):  
Antimicrobial Activity ◽  
Schiff Base ◽  
Metal Complexes ◽  
Dna Cleavage ◽  
Analytical Data ◽  
Amino Phenol ◽  
Ft Ir ◽  
Uv Visible ◽  
Schiff Base Metal Complexes

A series of novel (E)-2-((Tetrazolo[1,5-a]quinolin-4-ylmethylene)amino)phenol Cu(II), Co(II), Ni(II), Zn(II) and Mn (II) metal complexes have been synthesized 1:1 metal to ligand ratio, and these complexes were characterized by using analytical data such as FT-IR, UV-visible, Mass spectroscopy, SEM, EDX, TGA and magnetic moment measurements. The ligand and all the metal complexes were tested in vitro antimicrobial activity and DNA cleavage studies.

scholarly journals SYNTHESIS OF SOME 2,3-DIHYDRO-1,3,4-OXADIAZOLES AND 4,5-DIHYDRO-1,2,4-TRIAZOLES AS ANTICANCER AGENTS

2020 ◽  
pp. 92-99
Author(s):  
TAWFEEK A. YAHYA ◽  
JALAL H. ABDULLAH
Keyword(s):  
Cytotoxic Activity ◽  
Anticancer Agents ◽  
Colorimetric Assay ◽  
Human Cancer ◽  
Cancer Cell Line ◽  
Cytotoxic Activities ◽  
Standard Drug ◽  
Mass Spectral ◽  
Oxadiazole Derivatives

Objective: The main objective of this work was to synthesize and evaluate the novel 2,3-dihydro-1,3,4-oxadiazole and 4,5-dihydro-1,2,4-triazole derivatives for cytotoxic activities. Methods: The 2,3-dihydro-1,3,4-oxadiazole derivatives 4a-h were synthesized by cyclization of N'-(substituted-benzylidene) isonicotinohydrazide 3a-e in refluxing acetic anhydride. The 2,3-dihydro-1,3,4-oxadiazole derivatives 4a-h were converted into the corresponding 4,5-dihydro-1,2,4-triazoles 5a-h using ammonia. All the synthesized compounds were identified, depending on the physical and spectral data. Title compounds were assessed for their cytotoxic activity against human cancer cell line (MCF-7) by using Sulforhodamine B (SRB) colorimetric assay. Results: All the synthesized compounds showed characteristic peaks in FTIR, 1HNMR and Mass spectral analysis. The results of the in vitro cytotoxic activity revealed that the compound 4c exhibited equipotent cytotoxic activity with an IC50 value of 8.04 µM when compared with that of standard drug doxorubicin (IC50= 8.02 µM). The reminder compounds have shown good to moderate cytotoxic activities when compared with that of a reference standard. Conclusion: We synthesized a series of title compounds in quantitative yields. Most derivatives showed moderate to good cytotoxic activity.  

Synthesis and in vitro evaluation of substituted quinolines as new apoptosis inducers and anticancer agents: Pharmacophore-based design

2021 ◽  
Vol 18 ◽  
Author(s):  
Hiren Dayani ◽  
Abhishek Jha ◽  
Manjunath Ghate ◽  
Vivek K. Vyas
Keyword(s):  
Anticancer Agents ◽  
Caspase 3 ◽  
Cancer Cell Line ◽  
Pharmacophore Modeling ◽  
Design Synthesis ◽  
Substituted Quinolines ◽  
Activation Assay ◽  
Ic50 Values ◽  
Ft Ir

Background: Cancer is a global health burden and the leading cause of death across the world after cardiovascular disease. Objective: The objective of this work was the design, synthesis, and pharmacological evaluation of 2-phenylquinolin-4-amine derivatives as apoptosis inducers and anticancer agents. Method: In this study, we performed ligand-based pharmacophore modeling as a promising design strategy for the design of substituted quinoline derivatives as apoptosis inducers and anticancer agents. The designed compounds were synthesized as 2-phenylquinolin-4-amine derivatives and characterized by FT-IR, 1H-NMR, 13C-NMR, and Mass spectroscopy. Synthesized compounds were screened for apoptosis-inducing activity using caspase-3 activation and annexine-FITC assays and also screened against cancer cell line (HT-29) in an antiproliferative assay. Results: Synthesized compounds 7a and 7d demonstrated EC50 values of 6.06 and 6.69 µM in caspase-3 activation assay, respectively, and also showed late stage induction of apoptosis in annexine assay. Synthesized compounds 7a, 7d and 7i, also exhibited good antiproliferative activity with IC50 values of 8.12, 9.19, and 11.34 µM, respectively, which revealed that these are promising apoptosis inducers for the further development of new anticancer agents.

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.

Synthesis, SAR, In-Silico appraisal and Anti-Microbial Study of substituted 2-aminobenzothiazoles derivatives

2019 ◽  
Vol 15 ◽  
Author(s):  
Devidas G. Anuse ◽  
Suraj N. Mali ◽  
Bapu R. Thorat ◽  
Ramesh S. Yamgar ◽  
Hemchandra K. Chaudhari
Keyword(s):  
Antimicrobial Activity ◽  
In Silico ◽  
Docking Study ◽  
Moderate Activity ◽  
Molecular Docking Study ◽  
Mass Spectral ◽  
Gram Positive Bacteria ◽  
Ft Ir ◽  
In Silico Molecular Docking

Background: Antimicrobial resistance is major global health problem, which is being rapidly deteriorating the quality of human health. Series of substituted N-(benzo[d]thiazol-2-yl)-2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)acetamide (3a-j) were synthesized from substituted N-(benzo[d]thiazol-2-yl)-2-chloroacetamide/bromopropanamide (2a-j) and 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole (2) and further evaluated for their docking properties and antimicrobial activity. Methods: All synthesized compounds were characterized by FT-IR, NMR and Mass spectral analysis. All compounds were allowed to dock against different antimicrobial targets having PDB ID: 1D7U and against common antifungal target having PDB ID: 1EA1. Results: The compounds 3d and 3h were showed good activity against Methicillin-resistant Staphylococcus aureus (MRSA, resistance Gram-positive bacteria). All synthesized compounds showed good to moderate activity against selected bacterial and fungal microbial strains. If we compared the actual in-vitro antimicrobial activity and in-silico molecular docking study, we found that molecules 3i and 3h were more potent than the others. Conclusion: Our current study would definitely pave the new way towards designing and synthesis of more potent 2-aminobenzothiazoles derivatives.

scholarly journals Knigth's Move in the Periodic Table, From Copper to Platinum, Novel Antitumor Mixed Chelate Copper Compounds, Casiopeinas, Evaluated by an in Vitro Human and Murine Cancer Cell Line Panel

2001 ◽  
Vol 8 (1) ◽  
pp. 19-28 ◽  
Author(s):  
Isabel Gracia-Mora ◽  
Lena Ruiz-Ramírez ◽  
Celedonio Gómez-Ruiz ◽  
Mabel Tinoco-Méndez ◽  
Adriana Márquez-Quiñones ◽  
...  
Keyword(s):  
Cancer Cell ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Cancer Cell Line ◽  
Drug Candidates ◽  
Control Drug ◽  
Copper Compounds ◽  
Structure Activity ◽  
Cell Line Panel

We synthesized a novel anticancer agents based on mixed chelate copper (II) complexes, named Casiopeínas® has of general formula [Cu(N-N)(N-O)H2O]NO3 (where, N-N = diimines as 1,10- phenanthroline, 2,2-bipyridine, or substituted and N-O=aminoeidate or [Cu(N-N)(O-O)H2O]NO3 (where NN= diimines as 10-phenanthroline, 2,2-bipyridine or substituted Casiopeínas I, II, IV, V, VI, VII VIII and O-O=acetylacetonate, salicylaldehidate Casiopínas III). We evaluated the in vitro antitumor activity using a human cancer cell panel and some nurine cancer cells. Eleven Casiopeinas are evaluated in order to acquire some structure-activity correlations and some monodentated Casiopeinäs analogues; cisplatinum was used as control drug. The 50% growth inhibition observed is, in all cases reach with concentrations of Casiopeina's 10 or 100 times lower than cisplatinum. In a previous work we reported the induction of apoptosis by Casiopeina II. The results indicate that Casiopeinass are a promising new anticancer drug candidates to be developed further toward clinical trials.

scholarly journals Synthesis, Characterization, and Antimicrobial Activity of Methyl-2-aminopyridine-4-carboxylate Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
S. Nagashree ◽  
P. Mallu ◽  
L. Mallesha ◽  
S. Bindya
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Studies ◽  
H Nmr ◽  
Chemical Structures ◽  
Elemental Analyses ◽  
Ft Ir

A series of methyl-2-aminopyridine-4-carboxylate derivatives,3a–f,were synthesized in order to determine theirin vitroantimicrobial activity. The chemical structures of the synthesized compounds were confirmed by elemental analyses, FT-IR, and1H NMR spectral studies. Among the synthesized compounds,3cand3dshowed good antimicrobial activity compared to other compounds in the series.

scholarly journals Synthesis and Experimental Validation of New Designed Heterocyclic Compounds with Antiproliferative Activity versus Breast Cancer Cell Lines MCF-7 and MDA-MB-231

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Vincenza Barresi ◽  
Carmela Bonaccorso ◽  
Domenico A. Cristaldi ◽  
Maria N. Modica ◽  
Nicolò Musso ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Breast Cancer Cell Lines ◽  
Design And Synthesis ◽  
Human Breast Cell ◽  
Mcf 7

Recent drug discovery efforts are highly focused towards identification, design, and synthesis of small molecules as anticancer agents. With this aim, we recently designed and synthesized novel compounds with high efficacy and specificity for the treatment of breast tumors. Based on the obtained results, we constructed a Volsurf+ (VS+) model using a dataset of 59 compounds able to predict the in vitro antitumor activity against MCF-7 cancer cell line for new derivatives. In the present paper, in order to further verify the robustness of this model, we report the results of the projection of more than 150 known molecules and 9 newly synthesized compounds. We predict their activity versus MCF-7 cell line and experimentally verify the in silico results for some promising chosen molecules in two human breast cell lines, MCF-7 and MDA-MB-231.

scholarly journals SYNTHESIS AND CHARACTERIZATION IN VITRO ANTIMICROBIAL AND CYTOTOXICITY TESTING OF OXALIC ACID-DERIVED CADMIUM CHELATING AGENTS

2018 ◽  
Vol 10 (7) ◽  
pp. 80
Author(s):  
Daisy Selasteen F ◽  
Alfred Cecil Raj S ◽  
Alagappa Moses A
Keyword(s):  
Antimicrobial Activity ◽  
Silica Gel ◽  
Optical Conductivity ◽  
Cancer Cell Line ◽  
Uv Spectra ◽  
Diffusion Method ◽  
Spectral Studies ◽  
Cervical Cancer Cell Line ◽  
Cell Line Hela

Objective: The aim of this study is to investigate the growth, structure, spectral, solubility and biological activity of sodium cadmium oxalate dehydrate (NaCdOx) and cadmium oxalate trihydrate (CdOx) crystals prepared by a single diffusion method in the silica gel medium.Methods: The present crystals were grown using single diffusion methods and tested for XRD, UV absorption (190 to 1100 mm) and solubility (distilled water at 20-29 °C) studies. The antimicrobial efficacy of the grown samples at various concentrations (25, 50, 75 and 100 μg/ml) was studied against Streptococcus, (G+Ve), Pseudomonas aeruginosa (G-Ve) and Candida albicans (antifungal). The cytotoxicity evolution was carried out against human cervical cancer cell line (HeLa) using MTT assays.Results: The existing single crystals were successfully grown by silica gel technique. The solubility of sodium cadmium oxalate dehydrate (NaCdOx) was moderately good in deionized warm water. The FTIR spectral studies confirmed the chelating bands of the present samples and UV spectra showed the better the optical conductivity of as-grown crystals. The complexes showed good antimicrobial activity against all tested microbial strains and they exhibited a decrease in cytotoxicity activity.Conclusion: The gel method was suitable to grow metal complexes of legend crystals. The modification of structural properties of cadmium oxalate trihydrate (CdOx) by sodium doping was much improved the solubility, anticancer, antimicrobial activity and polarization by the high optical conductivity of sodium cadmium oxalate dehydrate (NaCdOx) compound. Hence sodium cadmium oxalate dehydrate (NaCdOx) might be a candidate for biomedical applications. 

scholarly journals SYNTHESIS AND STRUCTURAL ELUCIDATION OF AMINO ACETYLENIC AND THIOCARBAMATES DERIVATIVES FOR 2-MERCAPTOBENZOTHIAZOLE AS ANTIMICROBIAL AGENTS

2017 ◽  
Vol 9 (2) ◽  
pp. 192
Author(s):  
Aseel Alsarahni ◽  
Zuhair Muhi Eldeen ◽  
Elham Al-kaissi ◽  
Ibrahim Al- Adham ◽  
Najah Al-muhtaseb
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Antimicrobial Agents ◽  
Diffusion Method ◽  
Benzothiazole Derivatives ◽  
H Nmr ◽  
Ft Ir ◽  
Potential Antimicrobial Activity ◽  
C Nmr

<p><strong>Objective: </strong>To design and synthesize amino acetylenic and thiocarbonate of 2-mercapto-1,3-benthiazoles as potential antimicrobial agents.</p><p><strong>Methods: </strong>A new series of 2-{[4-(t-amino-1-yl) but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole derivatives (AZ1-AZ6), and S-1,3-benzothiazol-2-yl-O-alkyl carbonothioate derivatives were synthesised, with the aim that the target compounds show new and potential antimicrobial activity. The elemental analysis was indicated by the EuroEA elemental analyzer, and biological characterization was via IR, <sup>1</sup>H-NMR, [13]C-NMR, DSC were determined with the aid of Bruker FT-IR and Varian 300 MHz spectrometer using DMSO-d<sub>6</sub> as a solvent.<em> </em><em>In vitro </em>antimicrobial activity, evaluation was done for the synthesised compounds, by agar diffusion method and broth dilution test. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined. <em></em></p><p><strong>Results: </strong>The IR, <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, DSC and elemental analysis were consistent with the assigned structures. Compound of 2-{[4-(4-methylpiperazin-1-yl)but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole (AZ1), 2-{[4-(2-methylpiperidin-1-yl)but-2-yn-1-yl]sulfanyl}-1,3-benzothiazole (AZ2), 2-{[4-(piperidin-1-yl) but-2-yn-1-yl]sulfanyl}-1, 3-benzothiazole (AZ6), S-1,3-benzothiazol-2-yl-O-ethyl carbonothioate (AZ7), and S-1,3-benzothiazol-2-yl-O-(2-methylpropyl) carbonothioate (AZ9) showed the highest antimicrobial activity against <em>Pseudomonas aeruginosa </em>(<em>P. aeruginosa</em>), AZ-9 demonstrated the highest antifungal activity against <em>Candida albicans </em>(<em>C. albicans</em>), with MIC of 31.25 µg/ml.</p><p><strong>Conclusion: </strong>These promising results promoted our interest to investigate other structural analogues for their antimicrobial activity further.</p>

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