7720. Prednimustine

Nomenclature

CAS number: 29069-24-7
(11β)-21-[4-[4-[Bis(2-chloroethyl)amino]phenyl]-1-oxobutoxy]-11,17-dihydroxypregna-1,4-diene-3,20-dione; 11β,17,21-trihydroxypregna-1,4-diene-3,20-dione 21-[4-[p-[bis(2-chloroethyl)amino]phenyl]butyrate]; prednisolone 21-[4-[p-[bis(2-chloroethyl)amino]phenyl]butyrate]; Leo-1031; Sterecyt (Pharmaleo); Stereocyt (Bellon).
C35H45Cl2NO6; mol wt 646.64.
C 65.01%, H 7.01%, Cl 10.97%, N 2.17%, O 14.85%.

Description and references

Prednisolone ester of chlorambucil, q.v. Prepn: H. F. Fex et al., DE 2001305 corresp to US 3732260 (1970, 1973 both to AB Leo). In vitro study: A. H. Evenaar et al., Eur. J. Cancer 9, 773 (1973). Metabolism: R. Y. Kirdani et al., Oncology 35, 47 (1978). Clinical studies: L. Hakarsson et al., ibid. 103; J. E. Johnsson et al., Cancer Treat. Rep. 63, 421 (1970). Toxicity and antitumor activity study: K. R. Harrap et al., Eur. J. Cancer 13, 873 (1977). Series of articles on pharmacology, toxicology and clinical efficacy: Semin. Oncol. 13, Suppl. 1, 1-44 (1986).

Chemical structure

Properties

Crystals from methanol-water, mp 163-164°. [α]D24 +92.9° (c = 1.06 in chloroform).

Therapeutic Category

Antineoplastic.

Keywords

Antineoplastic; Alkylating Agents; Nitrogen Mustards