m-Carborane bisphenol structure as a pharmacophore for selective estrogen receptor modulators.

Abstract:

:A series of m-carborane derivatives was prepared based upon the structures of antiestrogenic drugs and their activities were evaluated by estrogen receptor alpha (ERalpha) binding assay and transactivation assay using human breast cancer cell line, MCF-7 cells. The m-carborane bisphenol 5 exhibited about a thousand times more potent ER agonistic activity than the o-carborane bisphenol 11. The m-carborane bisphenol structure appears to be a favorable hydrophobic pharmacophore for the development of novel selective estrogen receptor modulators (SERMs).

journal_name

Bioorg Med Chem Lett

authors

Ogawa T,Ohta K,Yoshimi T,Yamazaki H,Suzuki T,Ohta S,Endo Y

doi

10.1016/j.bmcl.2006.05.032

subject

Has Abstract

pub_date

2006-08-01 00:00:00

pages

3943-6

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(06)00574-9

journal_volume

16

pub_type

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