A new macrocyclic multidentate Schiff-base ligand Na4L consisting of two submacrocyclic units (10,21-bis-iminomethyl-3,6,14,17-tricyclo[17.3.1.18,12]tetracosa-1(23),2,6,8,10,12(24),13,17,19,21,-decaene-23,24-disodium) and its tetranuclear metal complexes with Mn(II), Co(II), Ni(II), Cu(II), and Zn(II) are reported. Na4L was prepared via a template approach, which is based on the condensation reaction of sodium 2,4,6-triformyl phenolate with ethylenediamine in mole ratios of 2 : 3. The tetranuclear macrocyclic-based complexes were prepared from the reaction of the corresponding metal chloride with the ligand. The mode of bonding and overall geometry of the compounds were determined through physicochemical and spectroscopic methods. These studies revealed tetrahedral geometries about Mn, Co, and Zn atoms. However, square planar geometries have been suggested for NiII and CuII complexes. Biological activity of the ligand and its metal complexes against Gram positive bacterial strain Staphylococcus aureus and Gram negative bacteria Escherichia coli revealed that the metal complexes become more potentially resistive to the microbial activities as compared to the free ligand. However, these metal complexes do not exhibit any effects on the activity of Pseudomonas aeruginosa bacteria. There is therefore no inhibition zone.

Aim: To investigate the cytotoxic effects of tamoxifen on the breast cancer cell line (MCF7). Methods:The cytotoxic effects of tamoxifen on MCF7 cells were investigated using caspase-9 activity and high content screening assays. Apoptosis mechanisms following tamoxifen treatment were also investigated. Results:The most significant cytotoxic effect of tamoxifen in MCF7 cells was a half-maximal inhibitory concentration (IC 50 ) of 4.506 µg/mL. A significant increase in caspase-9 activity was also observed when MCF7 cells were treated with tamoxifen (5 µg/mL). Furthermore, increased cell membrane permeability, cytochrome c level, and nuclear intensity were observed with tamoxifen (100 µg/mL) compared with doxorubicin (20 µg/mL) treatment. However, a noticeable decrease in cell viability and mitochondrial membrane permeability was observed with tamoxifen (100 µg/mL) treatment compared with doxorubicin (20 µg/mL) as a positive control. Conclusion:Tamoxifen showed in vitro cytotoxic effects in MCF7 cells as demonstrated by high-content screening and caspase-9 activity assays. Tamoxifen inhibits estrogen mechanisms, although toxic effect was observed.

Complexes of the type R2SnL2, where R = phenyl, butyl and methyl and LH = 2-thioacetic-5-phenyl-1,3,4-oxadiazole, have been synthesized and characterized by physico-chemical (elemental analysis, and electrolytic conductance) and spectral (UV-Visible, IR and (1H, 13C and 119Sn NMR) techniques. Monomer structures for the complexes, bidentate and octahedral geometry was proposed for the complexes prepared. Preliminary in vitro tests for fungicidal activity show that all prepared compounds display good activity to Gibberela, Cercospora arachidicola, Physolospora piricola and Fusarium oxysporum. Moreover, the Ph2SnL2 shows a higher inhibition percentage then diorganotin carboxylate.

New monomeric cobalt and cadmium complexes with Schiff-bases, namely, N′-[(E)-(3-hydroxy-4-methoxyphenyl)methylidene]furan-2-carbohydrazide (L1) and N′-[(E)-(3-hydroxy-4-methoxyphenyl)methylidene]thiophene-2-carbohydrazide (L2) are reported. Schiff-base ligands L1 and L2 were derived from condensation of 3-hydroxy-4-methoxybenzaldehyde (iso-vanillin) with furan-2-carboxylic acid hydrazide and thiophene-2-carboxylic acid hydrazide, respectively. Complexes of the general formula [M(L)2]Cl2 (where M = Co(II) or Cd(II), L = L1 or L2) have been obtained from the reaction of the corresponding metal chloride with the ligands. The ligands and their metal complexes were characterised by spectroscopic methods (FTIR, UV-Vis, 1H, and 13C NMR spectra), elemental analysis, metal content, magnetic measurement, and conductance. These studies revealed the formation of four-coordinate complexes in which the geometry about metal ion is tetrahedral. Biological activity of the ligands and their metal complexes against gram positive bacterial strain Bacillus (G+) and gram negative bacteria Pseudomonas (G−) revealed that the metal complexes become less resistive to the microbial activities as compared to the free ligands.

Multipara metric analysis of compound toxicity at the level of individual cells using flow cytometry and cellular imaging-based approaches such as High Content Screening (HCS) have played key roles in the detection of toxicity and classification of compounds based on observed patterns of reversible and irreversible cellular injury. Gold III complex (AuL 2 ) of bidentate ligand derived from the cyclization reaction of Schiff base of 4-amino-5-phenyl-4h-1,2,4-triazole-3-thiol with thioglycolic acid was synthesized and characterized by using melting point, FTIR spectroscopy, 1 HNMR, UV-Visible spectroscopy and elemental analysis. The presence of chloride counter ion in complex was supported by conductivity measurement and the presence of hydrated water was supported by thermal gravimetric studies. We examine the cytotoxic effects of gold complex and its ligand in one cultured cellular models (MCF7 cell line) by High Content Screening (HCS) and analysis and cell viability assay (MMT assay). The inhibitory effect of AuL 2 on breast cancer cell growth was due to induction of apoptosis as evidenced by annexin V staining and cell shrinkage. The study found that AuL 2 -mediated lead to disruption of Mitochondrial Membrane Potential (MMP), cell membrane permeability, nuclear condensation, fragmentation and release of cytochrome c from the mitochondria into the cytosol and also suggesting AuL 2 as a potential MCF7 inhibitor compared to doxorubicin as positive control. In this study, data showed that gold (III) complex AuL 2 may have therapeutic value in breast cancer treatment worthy of further development.