Synthesis, Characterization Of Platinum (Ⅱ) Complexes With 2,2-bis(Hydroxymethyl)-1,3-propane Acid As The Leaving Group

Since the discovery of antiproliferative activity of Cisplatin by Rosenberg in1965,six platinum-based drugs Cisplatin, Carboplatin, Oxaliplatin, Nedaplatin, Lobaplatin and Eptaplatin have been developed and approved for clinical application over past forty years, but the application is still greatly limited by severe toxicity of the drugs and resistance of cancer cells to the drugs. Therefore, the search for the new potent platinum complexes possessing high anti-tumour activity, low toxicity and lack of cross-resistance is continuing.A series of platinum(Ⅱ) complexes with 2,2-bis(hydroxymethyl)-1,3-propane acid as the leaving group and ammonia were synthesized and characterized by elemental analysis, FAB-MS,FT-IR,1H-NMR,¹³C-NMR and XRD spectroscopy in the paper. The carriers used were NH3, trans-1R,2R-diaminocyclo-hexane(DACH), ethylenediamine, (4R,5R)-4,5-bis-(aminomethyl)-2-ispropyl-1,3-dioxolane(BAMID), propanediamine, 2-hydroxy-1,3-propanediamine. The in vitro cytotoxicities of the complexes were assessed by sulforhodamine B (SRB) colorimetric assay.The results show that these compounds are in good agreement with the structures of the desired compounds. The compound LLC-1302 displays greater anticancer activity than Carboplatin, Oxaliplatin, and Eptaplatin against A549, HT-29, SCG-7901 cell lines, and is worth for further evaluation.