Synthesis of novel ligands for the stabilization of organometallic complexes having potential antitumor activity

Abstract

The design of new metal complexes as anticancer agents has received considerable interest in recent years. Complexes of titanium (e.g.: titanocene dichloride), lanthanides complexes (e.g.: texaphyrrins lanthanide) and carbenic complexes of gold, silver and copper showed significant biological activity, and have progressed into clinical trials. Thus, the target of this PhD project are the synthesis of new ligands and metal complexes. Firstly 5 cyclopentadienyl pro-ligands were synthesised: 6-phenylfulvene, 6-(p-metoxyphenyl)-fulvene e 6- (3',4'-dymethoxyphenyl)fulvene, 6-(3',5')-dymethoxyphenyl)fulvene and 6-(2',4')- dymethoxyphenyl)fulvene. Then, the synthesis of 12 novel scandium, yttrium and neodymium complexes with these cyclopentadienyl ligands was carried out. The complexes were tested on DU146 (Prostatic carcinoma) and MDA.MB213 (Breast cancer) to verify inhibition of cell-proliferation, using MTT test with standard procedures. All the complex showed a strong concentration-dependent ability of inhibiting the growth tumor cell, referring to antiblastic activity. [edited by author]