Synthesis, characterization, DNA/BSA binding and cytotoxicity studies of Mononuclear Cu(II) and V(IV) complexes of Mannich bases derived from Lawsone

2021 ◽  
pp. 131508
Author(s):  
Pratik Nariya ◽  
Falguni Shukla ◽  
Hitarthi Vyas ◽  
Ranjitsinh Devkar ◽  
Sonal Thakore
2014 ◽  
Vol 2014 ◽  
pp. 1-14 ◽  
Author(s):  
Pulipaka Ramadevi ◽  
Rinky Singh ◽  
Akhilesh Prajapati ◽  
Sarita Gupta ◽  
Debjani Chakraborty

A series of isonicotinoyl hydrazones have been synthesized via template method and were complexed to Cu(II). The ligands are coordinated to Cu(II) ion through the enolic oxygen and azomethine nitrogen resulting in a square planar geometry. The CT-DNA and bovine serum albumin binding propensities of the compounds were determined spectrophotometrically, the results of which indicate good binding propensity of complexes to DNA and BSA with high binding constant values. Furthermore, the compounds have been investigated for their cytotoxicities on A549 human lung cancer cell. Also the mode of cell death was examined employing various staining techniques and was found to be apoptotic.


Author(s):  
Emine Erdag

Aims: In this study, a series of new Mannich bases of 2(3H)-benzoxazolone derivatives containing substituted cyclic amine moieties with a potential to show cytotoxic activity have been prepared. In order to develop effective anticancer agents against various cancer cell lines, it is essential to study the structure activity relationship and the effect of different substituents on the activity of heterocyclic scaffolds which were known to have cytotoxic activities. Study Design: In silico and experimental design. Place and Duration of Study: Pharmaceutical Chemistry Department, Faculty of Pharmacy, Near East University, Nicosia, Cyprus, between January 2019- September 2020. Methodology: In this work, 2(3H)-benzoxazolone derivatives were prepared by Mannich reaction. The synthesis and structural characterization of the compounds were performed experimentally by FT-IR, 1H NMR, 13C NMR spectra and elemental analysis. In silico prediction of cell line cytotoxicity with PASS based CLC-Pred tool was performed to predict cytotoxicity of the compounds against different tumor cell lines. Results: In silico prediction results for the compounds showed that all benzoxazolone derivatives have cytotoxic activity against different cell lines and tumor types. It was clearly understood that the cytotoxicity of the compounds was affected by the substituents on their piperazine moieties and by the substituents on benzoxazolone core structure. Conclusion: In conclusion, newly synthesized Mannich bases of benzoxazolone derivatives were reported for the first time which may have a potential to show anticancer activities at different cancer cell lines. The efficiency of new compounds against cancer could be found via PASS based CLC-Pred database and could be further investigated by in vivo experimental cytotoxicity studies in the future to design new anticancer drug candidates.


2016 ◽  
Vol 453 ◽  
pp. 547-558 ◽  
Author(s):  
G . Kalaiarasi ◽  
C. Umadevi ◽  
A. Shanmugapriya ◽  
P. Kalaivani ◽  
F. Dallemer ◽  
...  

2020 ◽  
Vol 49 (13) ◽  
pp. 4100-4113 ◽  
Author(s):  
Surbhi Jain ◽  
Kishalay Bhar ◽  
Sandeep Kumar ◽  
Shreetama Bandyopadhyaya ◽  
Suman Tapryal ◽  
...  

In the current study, four novel mononuclear Cu(ii) complexes with terpyridine (L) and different co-ligands (phen, bipy, and imd) were synthesized and characterized in detail, where L is 4′-(3,4,5-trimethoxyphenyl)-2,2′:6′,2′′-terpyridine.


BioMetals ◽  
2017 ◽  
Vol 30 (4) ◽  
pp. 575-587 ◽  
Author(s):  
Qingming Wang ◽  
Han Mao ◽  
Wenling Wang ◽  
Huimin Zhu ◽  
Lihui Dai ◽  
...  

2019 ◽  
Vol 75 (8) ◽  
pp. 1091-1101
Author(s):  
K. T. Priya Vadhana ◽  
S. Parveen ◽  
B. Ushadevi ◽  
R. Selvakumar ◽  
S. Sangeetha ◽  
...  

A new set of differently hydrated barium and strontium squarates, namely poly[[triaqua(μ-1,2-dioxocyclobut-3-ene-1,2-diolato)barium] monohydrate], {[Ba(C4O4)(H2O)3]·H2O} n (1), poly[[diaqua(μ-1,2-dioxocyclobut-3-ene-1,2-diolato)strontium] monohydrate], {[Sr(C4O4)(H2O)2]·H2O} n (2), and poly[[triaqua(μ-1,2-dioxocyclobut-3-ene-1,2-diolato)barium/strontium(0.85/0.15)] monohydrate], {[Ba0.85Sr0.15(C4O4)(H2O)3]·H2O} n (3), is reported. The study of their crystal structures indicates that all the complexes crystallize in the triclinic space group P\overline{1}. Complexes 1 and 3 have a rare combination of squarate units coordinated through monodentate O atoms to two different metal atoms and through two bidentate O atoms to three different metal atoms. Furthermore, they have three coordinated water molecules to give a coordination number of nine. The squarate ligands in complex 2 exhibit two different coordination modes: (i) monodentate O atoms coordinated to four different Sr atoms and (ii) two monodentate O atoms coordinated to two different metal atoms with the other two O atoms bidentate to four different Sr atoms. All the compounds decompose to give the respective carbonates when heated to 800 °C, as evidenced by thermogravimetry/differential thermal analysis (TG-DTA), which are clusters of nanoparticles. Complexes 1 and 3 show additional endothermic peaks at 811 and 820 °C, respectively, indicating the phase transition of BaCO3 from an orthorhombic (α-Pmcn) to a trigonal phase (β-R3m). All three complexes have significant DNA-binding constants, ranging from 2.45 × 104 to 9.41 × 104 M −1 against EB-CT (ethidium bromide–calf thymus) DNA and protein binding constants ranging from 1.1 × 105 to 8.6 × 105 with bovine serum albumin. The in vitro cytotoxicity of the complexes is indicated by the IC50 values, which range from 128.8 to 261.3 µg ml−1. Complex 3 shows better BSA binding, antioxidant activity against the DPPH radical and cytotoxicity than complexes 1 and 2.


Ekologija ◽  
2010 ◽  
Vol 56 (3) ◽  
pp. 116-123 ◽  
Author(s):  
Janina Baršienė ◽  
Anne Bjornstad ◽  
Aleksandras Rybakovas ◽  
Janina Šyvokienė ◽  
Laura Andreikėnaitė

2016 ◽  
Vol 4 (11) ◽  
pp. 892-899
Author(s):  
AbdelKarim M. ◽  
◽  
Wafa O. ◽  
Nafesa A.G. ◽  
Inas O. ◽  
...  

Author(s):  
Muhammad Arfat Yameen ◽  
Amir Zeb ◽  
Raza E Mustafa ◽  
Sana Mushtaq ◽  
Nargis Aman ◽  
...  

Background: Incoherent use of antibiotics has led toward resistance in MRSA, which is becoming multidrugresistant with high rate of virulence in the community and hospital settings. Objective: Synergistic anti-MRSA activity was investigated in this study for hybrid material composite spheres of amoxicillin, Ag nanoparticles and chitosan which were prepared by one-step synthesis method and various characterizations were performed. Methods: Antimicrobial-susceptibility assay on MRSA was achieved by disc diffusion and agar dilution techniques while agar well diffusion was used for hybrid composite spheres. The in vitro and cytotoxicity studies was done by skin abrasion mouse model and MTT assay on RD cell respectively. Results: All isolates were resistant with the tested antibiotics except vancomycin. MIC against MRSA showed high resistance with amoxicillin from 4 to 128 mg L-1. The mean diameter of chitosan spheres and Ag nanoparticles was 02 mm and 277 nm respectively. Morphology of spheres was uneven, varied, porous and irregular in SEM and Ag nanoparticles presence and formation was also seen in micrograph. No substantial interface among drug, nanoparticles and polymer was found in XRD and IR showed characteristic peaks of all compound in the formulation. The in vitro assay showed augmented anti-MRSA activity with amoxicillin loaded hybrid composite spheres (22-29 mm). A significant reduction in microbial burden (~6.5 log10 CFU ml-1) was seen in vivo with loaded hybrid composite spheres formulation. The MTT assay indicated no potential cytotoxicity with hybrid composite spheres. Conclusion: Synergistic effect, amoxicillin, new hybrid formulation, anti-MRSA activity, composite spheres. nanoparticles.


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