Synthese Und Antitumoraktivität Von Platin(II)-Komplexen Mit Cholesterinderivaten

✍ Scribed by H. Brunner; G. Sperl

• Publisher: Wiley (John Wiley & Sons)
• Year: 2010
• Weight: 437 KB
• Volume: 101
• Category: Article
• ISSN: 0037-9646
• DOI: 10.1002/bscb.19921011106

✦ Synopsis

Abstract

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 PtCl~2~ fragment via their NH~2~ 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(NH~3~)~2~ fragment. The antitumor activity of the compounds was tested towards the lymphatic P 388 leukemia of the CD~2~F~1~ mouse and towards the human mammary carcinoma cell line MDA‐MB 231. The Pt(II) complexes gave a maximum growth inhibition of 54%.