Bioactive fragments synergically involved in the design of new generation Pt(ii) and Pd(ii)-based anticancer compounds.
New Pt(ii) and Pd(ii) complexes with the metal center coordinated to two different chelating ligands, tropolone (trop) and dihexadecyl-2,2'-bipyridine-4,4'-dicarboxylate bipyridine (bipy), [(bipy)M(trop)][CF(3)SO(3)], have been synthesized and their biological evaluation has been performed demonstrating a remarkable cytotoxic activity in vitro against the human prostate DU145 and hormone-sensitive LNCaP cells lines. Moreover, for the Pt(ii) derivative, the molecular structure has been determined by single-crystal X-ray diffraction and computational analysis on the hydrolysis reaction mechanisms have been performed by density functional theory (DFT) calculations, in order to correlate molecular structure, biological activity and mechanism of action of this new class of complexes based on two different bioactive fragments.
Pucci
Daniela
D
Centro di Eccellenza CEMIF, CAL-LASCAMM, Unità INSTM della Calabria, Dipartimento di Chimica Università della Calabria, 87030, Arcavacata di Rende (CS), Italy. d.pucci@unical.it
Bellusci
Anna
A
Bernardini
Sergio
S
Bloise
Rossana
R
Crispini
Alessandra
A
Federici
Giorgio
G
Liguori
Paola
P
Lucas
Maria Fatima
MF
Russo
Nino
N
Valentini
Alessandra
A
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D018360:Crystallography, X-Ray; D006801:Humans; D006868:Hydrolysis; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D015394:Molecular Structure; D010165:Palladium / Q000737:chemistry*; D017671:Platinum Compounds / Q000737:chemistry* / Q000494:pharmacology*
D000970:Antineoplastic Agents; D017671:Platinum Compounds; D010165:Palladium