6230. Mofarotene

Nomenclature

CAS number: 125533-88-2
4-[2-[4-[(1E)-2-(5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl]phenoxy]ethyl]morpholine; Ro 40-8757.
C29H39NO2; mol wt 433.63.
C 80.32%, H 9.07%, N 3.23%, O 7.38%.

Description and references

Anticancer aromatic analog of retinoic acid (arotinoid). Prepn: M. Klaus et al., EP 331983; eidem, US 4940707 (1989, 1990 both to Hoffmann-La Roche). Mode of action study: J. F. Eliason et al., Blood 86, 4516 (1995). Pharmacokinetics: B. Vallès et al., Eur. J. Drug Metab. Pharmacokinet. 20, 49 (1995). HPLC determn in plasma: R. Wyss et al., J. Chromatogr. A 729, 315 (1996). Mechanism of growth inhibition on pancreatic cancer cells: S. Kawa et al., Int. J. Cancer 72, 906 (1997). Clinical pharmacology in combination with cisplatin and etoposide: L. van Zuylen et al., Anti-Cancer Drugs 10, 361 (1999).

Chemical structure

Properties

White crystals from ethyl acetate/hexane, mp 107-109°.

Therapeutic Category

Antineoplastic.

Keywords

Antineoplastic; Retinoids and Analogs