Complexes of palladium(II) with 1-phenyl-1-hydroxymethylene bisphosphoniс acid and their antitumor activity

Abstract

complex formation of K 2 [Pdcl 4 ] with 1-phenyl-1-hydroxymethylene bisphosphonic acid (PhhMBP, h 4 K e y w o r d s: palladium(II) complexes, bisphosphonic acid, cytotoxic activity, toxicity.C isplatin is still one of the most famous and efficient anticancer drugs used in the clinical practice [1]. Nevertheless, searching for new compounds with antineoplastic action continues to eliminate the serious side effects, to improve the clinical efficacy and to broaden the antitumor spectrum. In particular, palladium(II) bisphosphonates are promising species for the treatment of bone cancer and metastases: complexes include a cytotoxic metal (palladium) and a bisphosphonic acid, which possesses affinity for bone tissue and can ensure targeted delivery of the cytotoxic metal to the lesion site [2][3][4][5][6][7][8][9]. The P-C-P moiety present in bisphospho nic acids provides their active link to the bone matrix, and two side substituents determine their physicochemical and pharmacologic properties. To study the effect of the structure of complex and chemical nature of the substituents bonded to the carbon atom of bisphosphonate moiety on the biological activity, the formation of palladium(II) complexes with 1-phenyl-1-hydroxymethylene bisphosphoniс acid was investigated, which, besides two phosphonic groups, contain a hydroxy group and a phenyl moiety.