Synthesis And Anti-tumor Activity Of Chalcone Derivatives And Their Pt(IV) Complexes

Chalcones are a class of natural organic compounds existed in medicinal plants, whichare the precursors to synthesize flavones. The main structure of chalcone is 1,3-bis-aryl-prop-2-en-1-one. The structure of chalcone is flexible, so it can bind different receptors. However,the source of natural chalcones is very limited, so it is very import to study the synthesis ofchalcones. This article summarizes the synthesis of chalcones and its application. We use 2-acetyl pyridine and substituted benzaldehyde as reactants, and use sodium carbonate ascatalyst to synthesize a series of aza-chalcones in aqueous, the yield are 65%-97%. We discussthe effect of solvent and system to the reaction. Compared with classical method, the mainadvantages of the present procedure are higher yields and environment-friendly.Thiosemicarbazone Schiff bases have significantly activity of antibacterial, antitubercular,antitumor, anti-fungal, anti-HIV, anti-convulsant, anti-oxidation and so on. And its moleculestructure contains S and N atom, which have strong coordination capacity, so it can provideelectronic to form chelates with metal ions. Because of its coordination atoms is the same assome biological ligands, the pharmacological activity will stronger than before formedcomplexes with metal. We use chalcones and thiosemicarbazide hydrochloride salt tosynthesize chalcone thiosemicarbazone Schiff base in the presence of sodium acetate underultrasonic irradiation at room temperature, the yields are 67%-87%, and we discuss the effectof solvent, reactant and condition to the reaction. Compared with reported method, the mainadvantages of the present procedure are higher yields and shorter reaction time.Platinum complexes are the most widely used in the treatment of malignant tumors, it iswell known that the universality and validity of anti-tumor. However, their serious toxic sideeffect has restricted the application of these drugs. To overcome these disadvantages, peoplehave explored to prepare many new platinum complexes and studied their anti-tumor activityin recent decades. In these study, Pt(IV) complexes and the complexes which have biologicalactivities become the focus. In this paper, we prepare some Pt(IV) complexes with azachalcones,and characterize their structure, and test the anti-tumor activity of human lung cancer cell(A-549) and human cervical carcinoma cell(Hela). The results show that thesecomplexes have inhibition of A-549 cells, and some of these have inhibition of Hela cells, andthe corresponding ligands have no inhibition except 3-(4-nitrophenyl)-1-(pyridine-2-yl)prop-2-en-1-one.