Synthesis,Structures And Cytotoxicity Studies Of Ruthenium, Rhodium, Iridium, Complexes With Curcuminoids

Curcumin is the major active component extracted from the roots of turmeric Recently, curcumin has attracted increasing attentions for its extensive pharmacological activit expecially the excellent anticancer effect and low cytotocity. As a result, curcumin has been listed as the third generation medicine for cancer chemoprevention. But the amount of natural curcumin is less, and the cost is expensive. Thus, the curcumin compound with antitumor activity is synthesized to improve the shortcomings of the natural curcumin.Curcumin is a very good type of two ligands, and it has some anticancer activity and even higher than the ligand itself.. This suggests that the compounds of the curcumin compounds-organic metal complexes are potential applications for anticancer drugs.Our research work mainly focuses on the following aspects:1.Synthesis and characterization of curcuminoids We obtained 9 kinds of curcuminoids ligands by the reaction of acetyl and acetone as raw material with benzodiazepine aldehyde(heterocyclic aldehydes).We used 1H NMR spectrum to characterize the 9 ligands. Among them, the absolute configurations of ligand L1, L2, L6, L7 were determined by X-ray single crystal diffraction.2.Synthesis and characterization of ruthenium, rhodium, iridium organometallic complexes containing curcuminoidsWe obtain 23 new complexes by the reaction of the above 9 curcuminoids ligands with [Ru(η6-p-cymene)Cl2]2, [Rh(η5-C5(CH3)5)Cl2]2, [Ir(η5-C5(CH3)5)Cl2]2. These complexes are characterized by 1H NMR, 13 C NMR, MS and elemental analysis. The absolute configurations of complexes 1, 2, 3, 6 were determined by X-ray single crystal diffraction.3. antitumor activity of curcuminoids and the corresponding organometallic complexesWe used the MTT method to determine in vitro growth inhibitory activity of complexes 1, 2 against Hela, BEL-7404, SMMC-7721 and HEK-293 T.The results showed that the two complexes exhibited moderate activity against these three kinds of cancer cells and showed greater toxicity against the normal HEK-293 T cells, which indicated that the two complexes have no selectivity for the cells. Similarly,we investiaged the in vitro activity of the ligand L4~L9, curcumin and 3~23 complexes. All compounds showed certain toxicity against cancer cells and showed greater toxicity to normal cells.The values of complex 15 are and against and cancer cell lines, respectively, while that is 25 against normal cell lines, which indicates the good selectivity of this complex.