Palladium(II)/ N , N -disubstituted- N ′-acylthioureas complexes as anti- Mycobacterium tuberculosis and anti- Trypanosoma cruzi agents

Abstract

The new complexes of Pd(II) with N,N-disubstituted-N 0-acylthioureas:[(1) [Pd(dppf)(N,N-dimethyl-N 0benzoylthioureato-k 2 O,S)]PF 6 , (2) [Pd(dppf)(N,N-diethyl-N 0-benzoylthioureato-k 2 O,S)]PF 6 , (3) [Pd(dppf) (N,N-dibuthyl-N 0-benzoylthioureato-k 2 O,S)]PF 6 , (4) [Pd(dppf)(N,N-diphenyl-N 0-benzoylthioureato-k 2 O, S)]PF 6 , (5) [Pd(dppf)(N,N-diethyl-N 0-furoylthioureato-k 2 O,S)]PF 6 , (6) [Pd(dppf)(N,N-diphenyl-N 0-furoylthioureato-k 2 O,S)]PF 6 , (7) [Pd(dppf)(N,N-dimethyl-N 0-thiophenylthioureato-k 2 O,S)]PF 6 , and (8) [Pd(dppf) (N,N-diphenyl-N 0-thiophenylthioureato-k 2 O,S)]PF 6 , were prepared and characterized by elemental analysis, and spectroscopic techniques. The structures of complexes (2), (3), (5), (6) and (8) had their structures determined by X-ray crystallography, confirming the coordination of the ligands with the metal through sulfur and oxygen atoms, forming distorted square-planar geometries. These complexes have shown antibacterial activity against anti-Mycobacterium tuberculosis H37Rv ATCC 27294. The complexes exhibited antiparasitic activity against Trypanosoma cruzi, while the metal-free thioureas did not. The results demonstrated that the compounds described here can be considered as promising anti-Mycobacterium tuberculosis and anti-T. cruzi agents, since in both cases their in vitro activity were better than reference drugs available for the treatment of both diseases.

The trans -[Ru(PPh 3 ) 2 ( N , N -dimethyl- N ′-thiophenylthioureato-k 2 O,S)(bipy)]PF 6 complex has pro-apoptotic effects on triple negative breast cancer cells and presents low toxicity in vivo

“…Results demonstrate that complex (2) exhibited the highest SI, with the lowest IC 50 for MDA-MB-231 cells (8.81 ± 0.81 μM) and the highest IC 50 for MCF-10A (14.82 ± 2.50 μM) demonstrating to be the most effective among the three complexes tested. The results of this assay are in accordance with another work of the group where the smallest ligands were more active [45]. Thus, complex (2) was selected to be further investigated using in vitro and in vivo assays.…”

Synthesis, in vitro and in vivo biological evaluation, COX-1/2 inhibition and molecular docking study of indole-N-acylhydrazone derivatives

“…The CC 50 values were calculated on the GraphPad Prism version 5.0, San Diego California, USA. 40 4.2.1.2. Lymphoproliferation assay.…”

Search for new drugs as pharmacological targets

“…The in vitro antitumor activity of the ligands and their metal complexes were evaluated tumor cells DU-145 (prostate cancer cells), (MDA-MB-231 (breast cancer cells), L929 (healthy cells of mouse), antibacterial against strains of M. tuberculosis H37Rv and antiparasitic against epimastigotes of Trypanosoma cruzi. Of the exposed results, eight of the thirty-two metal complexes were active against the evaluated targets [6][7][8].…”