Enhancement in intramolecular interactions and in vitro biological activity of a tripodal tetradentate system upon complexation

2015 ◽  
Vol 44 (35) ◽  
pp. 15591-15601 ◽  
Author(s):  
Nidhi Tyagi ◽  
Mambattakkara Viji ◽  
Suneesh C. Karunakaran ◽  
Sunil Varughese ◽  
Shilpa Ganesan ◽  
...  
Keyword(s):  
Biological Activity ◽  
Metal Complexes ◽  
Anticancer Activity ◽  
Intramolecular Interactions

Naphthalimide appended metal complexes uniquely exhibited intramolecular interactions, affinity for DNA/proteins and apoptosis mediated anticancer activity.

scholarly journals Novel Papaverine Metal Complexes with Potential Anticancer Activities

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5447
Author(s):  
Ahmed Gaber ◽  
Walaa F. Alsanie ◽  
Deo Nandan Kumar ◽  
Moamen S. Refat ◽  
Essa M. Saied
Keyword(s):  
Breast Cancer ◽  
Biological Activity ◽  
Metal Complexes ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Anticancer Activities ◽  
Mcf 7

Cancer is one of the leading causes of death worldwide. Although several potential therapeutic agents have been developed to efficiently treat cancer, some side effects can occur simultaneously. Papaverine, a non-narcotic opium alkaloid, is a potential anticancer drug that showed selective antitumor activity in various tumor cells. Recent studies have demonstrated that metal complexes improve the biological activity of the parent bioactive ligands. Based on those facts, herein we describe the synthesis of novel papaverine–vanadium(III), ruthenium(III) and gold(III) metal complexes aiming at enhancing the biological activity of papaverine drug. The structures of the synthesized complexes were characterized by various spectroscopic methods (IR, UV–Vis, NMR, TGA, XRD, SEM). The anticancer activity of synthesized metal complexes was evaluated in vitro against two types of cancer cell lines: human breast cancer MCF-7 cells and hepatocellular carcinoma HepG-2 cells. The results revealed that papaverine-Au(III) complex, among the synthesized complexes, possess potential antimicrobial and anticancer activities. Interestingly, the anticancer activity of papaverine–Au(III) complex against the examined cancer cell lines was higher than that of the papaverine alone, which indicates that Au-metal complexation improved the anticancer activity of the parent drug. Additionally, the Au complex showed anticancer activity against the breast cancer MCF-7 cells better than that of cisplatin. The biocompatibility experiments showed that Au complex is less toxic than the papaverine drug alone with IC50 ≈ 111 µg/mL. These results indicate that papaverine–Au(III) complex is a promising anticancer complex-drug which would make it a suitable candidate for further in vivo investigations.

Computational Druglikeness Assessment, Synthesis, Characterization and in vitro Biological Activity Evaluation of some Novel Mixed Metal Complexes of 2-(butan-2-ylidene) hydrazinecarbothioamide

2020 ◽  
Vol 23 ◽  
Author(s):  
Tahmeena Khan ◽  
Iqbal Azad ◽  
Alfred J. Lawrence ◽  
Saman Raza ◽  
Seema Joshi ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Molecular Docking ◽  
Metal Complexes ◽  
Docking Studies ◽  
Mixed Metal ◽  
Ic50 Value ◽  
Mixed Metal Complexes ◽  
Mcf 7

Aims and Objectives: The heteronuclear (mixed metal) complexes of Schiff bases have been explored as part of the coordination and bioinorganic chemistry. Five novel mixed metal complexes of (E)-2-(butan-2-ylidene) hydrazinecarbothioamide (2-butanone thiosemicarbazone) were prepared and characterized by different spectroscopic techniques. Molecular docking studies were performed with three proteins for two complexes. The toxicity potential, physicochemical properties and bioactivity scores were also predicted. The complexes were tested against three cell lines and also evaluated for their antibacterial activity. Materials and Methods: The mixed metal complexes were prepared in 1:4 molar ratio of metal salt and ligand. OSIRIS 4.6.1 was used to assess the toxicity whereas Molinspiration 2016.03 was used to calculate the bioactivity scores and other physicochemical properties. Principal Component Analysis (PCA) was performed using the Osiris Property Explorer 4.5.1 for defining and visualizing multidimensional property spaces by assigning dimensions to numerical descriptors. Molecular docking studies were performed with three proteins. The anticancer activity was tested against MCF-7, MDA-MB-231, HepG2 and A549 cell lines using MTT assay whereas antibacterial activity was tested using disc diffusion method. Results and Conclusion: The melting points of the complexes were as high as >3500C, indicating high thermal stability. [CuZn(C5H11N3S)4(SO4)2] exhibited minimum energies against the selected proteins. The bioactivity scores of the complexes were between -0.50 and 0.0. All the prepared complexes showed negative Ames score predicted their non-carcinogenic nature. Against A549 [CuZn(C5H11N3S)4(SO4)2], [CoZn(C5H11N3S)4(SO4)Cl2] and [FeZn(C5H11N3S)4(SO4)2] showed potential in vitro activity. IC50 of these three complexes were 19.69, 37.73 and 38.4 respectively. Against MCF-7, [FeCu(C5H11N3S)4(SO4)2] had IC50 value 53.5. Whereas, against HepG2 [CoZn(C5H11N3S)4(SO4)Cl2] was active having IC50 value 61.8. [CoZn(C5H11N3S)4(SO4)Cl2], [FeCu(C5H11N3S)4(SO4)2] and [FeCo(C5H11N3S)4(SO4)Cl2] were active against S. aureus in the concentration range 2-20 mg/mL. The complexes showed improved biological activity as compared to the monometallic complexes of the same ligand.

In vitro biological activity of copper(II) complexes with NSAIDs and nicotinamide: Characterization, DNA- and BSA-interaction study and anticancer activity

2021 ◽  
pp. 111696
Author(s):  
Flóra Jozefíková ◽  
Spyros Perontsis ◽  
Katarína Koňáriková ◽  
Ľubomír Švorc ◽  
Milan Mazúr ◽  
...  
Keyword(s):  
Biological Activity ◽  
Anticancer Activity ◽  
Interaction Study ◽  
Bsa Interaction

scholarly journals 1,3,4-Thiadiazole Derivatives. Part 91. Synthesis and Biological Activity of Metal Complexes of 5-(2-Aminoethyl)-2-Amino-1,3,4-Thiadiazole

1996 ◽  
Vol 3 (5) ◽  
pp. 227-232 ◽  
Author(s):  
Mihai Barboiu ◽  
Marilena Cimpoesu ◽  
Cornelia Guran ◽  
Claudiu T. Supuran
Keyword(s):  
Biological Activity ◽  
Antifungal Activity ◽  
Metal Complexes ◽  
Elemental Analysis ◽  
Electronic Spectroscopy ◽  
Candida Spp ◽  
Thiadiazole Derivatives ◽  
In Vitro Antifungal Activity

Metal complexes of the title ligand (L) containing Co(II), Ni(II) and Cu(II) were prepared and characterized by elemental analysis, IR, electronic spectroscopy and conductimetry. The new derivatives, possessing the following formulae, CuL2(OH)2, NiL2Cl2, and [Co2LCl4]n showed in vitro antifungal activity against Aspergillus and Candida spp.

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