SYNTHESIS AND ANTITUMOR-ACTIVITY OF PLATINUM(II) COMPLEXES WITH CHOLESTEROL DERIVATIVES

Low-density-lipoprotein-receptor binding moieties were introduced into Pt(II) complexes in order to facilitate the selective transport into cancer cells. Cholesterol esters of aminoacids and 2,3-diaminopropionic acid were attached to the PtCl2 fragment via their NH2 groups. Steroidal amine and diamine ligands were synthesized and transformed into the corresponding dichloroplatinum(II) complexes. A steroidal carboxylic acid was prepared and coupled with the Pt(NH3)2 fragment. The antitumor activity of the compounds was tested towards the lymphatic P 388 leukemia of the CD2F1 mouse and towards the human mammary carcinoma cell line MDA-MB 231. The Pt(II) complexes gave a maximum growth inhibition of 54%.