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Title:
AFFINITY LABEL TO STEROID HORMONE RECEPTOR, AND APPLICATION AS CONTRAST MEDIUM FOR HORMONE RADIOTHERAPY AND HORMONE DEPENDENT CANCER
Document Type and Number:
Japanese Patent JPH02138294
Kind Code:
A
Abstract:

NEW MATERIAL: An affinity label consists of a ligand which is specific and irreversible to a steroid hormone receptor. The label is composed of an estrogen complex constituted by an estradiol derivative which is complexed with an organometallic compound at the 17α-position of estradiol. In the affinity label, PK which measures an equilibrium constant between an alcohol at the 17β-position of the complex and carbenium forms at 17-position is negative.

EXAMPLE: 17α-Pherocenyl-17β-estradiol of formula I.

USE: Drugs for hormone radiotherapy of hormone dependent cancer, contrast medium for hormone dependent cancer.

PROCESS: For example, a compound of formula II which is prepared by silylating estrone with dimethyl-tert-butylchlorosilane is added with the lithium derivative of pherocene of formula III to obtain the compound of EXAMPLE.


Inventors:
JIERAARU JIYAUAN
ANNU BESHIEERU
Application Number:
JP13901389A
Publication Date:
May 28, 1990
Filing Date:
May 31, 1989
Export Citation:
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Assignee:
IERUEESERUTAAGU SA
CENTRE NAT RECH SCIENT
International Classes:
G01N33/60; A61K31/565; A61K47/02; A61K49/04; A61K51/04; A61P35/00; C07B59/00; C07J1/00; C07J51/00; C07J75/00; G01N33/74; (IPC1-7): A61K31/565; A61K47/02; A61K49/04; C07B59/00; C07J1/00; C07J75/00; G01N33/60; G01N33/74
Attorney, Agent or Firm:
Kazuo Sato (2 outside)