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

BRUNNER, H and SPERL, G (1992) SYNTHESIS AND ANTITUMOR-ACTIVITY OF PLATINUM(II) COMPLEXES WITH CHOLESTEROL DERIVATIVES. BULLETIN DES SOCIETES CHIMIQUES BELGES, 101 (11). pp. 935-943. ISSN 0037-9646,

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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 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%.

Item Type: Article
Uncontrolled Keywords: CELL-LINES; LIGANDS; ESTERS;
Depositing User: Dr. Gernot Deinzer
Last Modified: 19 Oct 2022 08:44
URI: https://pred.uni-regensburg.de/id/eprint/54299

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