title: 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).
authors.affiliation: Faculty of Pharmaceutical Sciences, Tohoku Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai 981-8558, Japan.
authors.forename: Takumi
authors.initials: T
authors.lastname: Ogawa
authors.forename: Kiminori
authors.initials: K
authors.lastname: Ohta
authors.forename: Tomohiro
authors.initials: T
authors.lastname: Yoshimi
authors.forename: Hiroto
authors.initials: H
authors.lastname: Yamazaki
authors.forename: Tomoharu
authors.initials: T
authors.lastname: Suzuki
authors.forename: Shigeru
authors.initials: S
authors.lastname: Ohta
authors.forename: Yasuyuki
authors.initials: Y
authors.lastname: Endo
mesh_terms: D001559:Benzhydryl Compounds; D001667:Binding, Competitive; D001896:Boron Compounds / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D010636:Phenols / Q000737:chemistry* / Q000494:pharmacology*; D020845:Selective Estrogen Receptor Modulators / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D000098851:Carboranes
chemical_list: D001559:Benzhydryl Compounds; D001896:Boron Compounds; D010636:Phenols; D020845:Selective Estrogen Receptor Modulators; C513207:m-bis(hydroxyphenyl)carborane; D000098851:Carboranes