3446. Droloxifene

Nomenclature

CAS number: 82413-20-5
3-[(1E)-1-[4-[2-(Dimethylamino)ethoxy]phenyl]-2-phenyl-1-butenyl]phenol; (E)-α-[p-[2-(dimethylamino)ethoxy]phenyl]-α′-ethyl-3-stilbenol; (E)-1-[4′-(2-dimethylaminoethoxy)phenyl]-1-(3-hydroxyphenyl)-2-phenylbut-1-ene; 3-hydroxytamoxifen.
C26H29NO2; mol wt 387.51.
C 80.59%, H 7.54%, N 3.61%, O 8.26%.

Description and references

Estrogen-receptor antagonist. Prepn: H. Schickaneder et al., EP 54168; eidem, US 5047431 (1982, 1991 both to Klinge); P. C. Ruenitz et al., J. Med. Chem. 25, 1056 (1982). Symposium on pharmacology and clinical studies: Am. J. Clin. Oncol. 14, Suppl. 2, S1-S63 (1991). Clinical trial in breast cancer: P. F. Bruning, Eur. J. Cancer 28A, 1404 (1992).

Chemical structure

Properties

Colorless crystals from ether, mp 162-163° (Schickaneder); also reported as white crystals from benzene-hexane, mp 160-162° (Ruenitz).

Derivative

Citrate.

Nomenclature

CAS number: 97752-20-0
K-21060E; FK-435.
C26H29NO2.C6H8O7; mol wt 579.64.
C 66.31%, H 6.43%, N 2.42%, O 24.84%.

Properties

Slightly sol in water, methanol, ethanol. Insol in chloroform.

Therapeutic Category

Antineoplastic (hormonal).

Keywords

Antineoplastic (Hormonal); Antiestrogens; Selective Estrogen Receptor Modulator (SERM)