In vitro antileukemia, antibacterial and antifungal activities of some 3d metal complexes: Chemical synthesis and structure – activity relationships

Abstract

The present paper describes the synthesis, characterization and in vitro biological evaluation screening of different classes (ammoniacates, dioximates, carboxylates, semi-and thiosemicarbazidates) of Co(II), Co(III), Cu(II), Ni(II), Mn(II), Zn(II) and Fe(III) complexes. Schiff bases were obtained from the reaction of some salicyl aldehydes with, respectively, furoylhydrazine, benzoylhydrazine, semicarbazide, thiosemicarbazide and S-methylthiosemicarbazide to give tridentate ligands containing ONO, ONS or ONN as donor atoms. The synthetic metal complexes are of various geometrical and electronic structures, thermodynamic and thermal stabilities, and magnetic and conductance properties. All complexes, except those of Cu, are octahedral. Some Cu, Co and Mn compounds have a dimeric or a polymeric structure. The composition and structure of complexes were analysed by elemental analysis, IR and 1 H NMR and 13 C NMR spectroscopies, and magnetochemical, thermoanalytical and molar conductance measurements. All ligands and metal complexes were tested as inhibitors of human leukemia (HL-60) cells growth, and the most potent, the Cu(II) complexes, have been also tested for their in vitro antibacterial and antifungal activities. Structure-activity relationships were carried out.

Synthesis, characterization, crystal structure of novel Cu (II), Co (III), Fe (III) and Cr (III) complexes with 2‐hydroxybenzaldehyde‐4‐allyl‐S‐methylisothiosemicarbazone: Antimicrobial, antioxidant and in vitro antiproliferative activity

“…The Cu(1) atom in 3 is penta-coordinated in a distorted square-pyramidal coordination geometry. The octahedral volumes of Co atoms in 5 and 6 are equal to 9.151 and 9.076 Å 3 , whereas for Fe (7,8) and Cr (9) atoms the corresponding values are 10.994, 10.982, and 10.364 Å 3 , respectively. The apex of the metal's coordination pyramid in 3 is occupied by oxygen atom O(2 W) of another H 2 O molecule with a distance of 2.312(5) Å.…”

“…calcd for C 12 2.3 | General procedure for the preparation of the metal complexes (1)(2)(3)(4)(5)(6)(7)(8)(9) All the new metal complexes 1-9 were prepared by the direct reaction between the ligand and the corresponding metal salts. : 142-144°C; yield (83%); FW: 249.332 g mol −1 .…”

“…[1][2][3][4][5][6][7] In recent years, a number of thiosemicarbazone derivatives have been synthesized, and their biological activities were also evaluated. [1][2][3][4][5][6][7] In recent years, a number of thiosemicarbazone derivatives have been synthesized, and their biological activities were also evaluated.…”

Complex‐Formation Ability of Salicylaldehyde Thiosemicarbazone towards ZnII, CuII, FeII, FeIII and GaIII Ions

“…[6,8] The presence of a phenol OH group at a chelatable position like in the salicylaldehyde (or 2-hydroxybenzaldehyde) thiosemicarbazone (STSC, H 2 L; Scheme 1) instead of the pyridyl nitrogen atom might provide a different and more favourable coordination for harder metal ions that prefer oxygen donor atoms. [10] For example, a monomeric Cu II complex of STSC showed distinct activity on a human leukemia cell line [12] and Zn II complexes of various derivatives of STSC display considerable antimicrobial activity. [10] For example, a monomeric Cu II complex of STSC showed distinct activity on a human leukemia cell line [12] and Zn II complexes of various derivatives of STSC display considerable antimicrobial activity.…”

Substituted 1,3-Phenyl(Pyridyl) Propenones and Derivatives with Thiosemicarbazidic Groups. Structrure – (HL-60) Antileukemia Activity Relationship

“…It was identifi ed that for compound 10a with two pyridine nuclei the inhibitor activity decrease slower when is diluted and achieves ~60% at concentration of 10 -7 mol/L. The high anticancer activity for compound 10a can be explained by the formation of the strong hydrogen bonds between the inhibitor and the nucleic acid of the cancer cells [13].…”