Steroid derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai

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540 94, A61K 3158, C07J 1700

Patent

active

057122636

ABSTRACT:
To provide novel steroid derivatives having an antitumor action which can be synthesized efficiently and stereoselectively by means of synthetic organic chemistry. A steroid derivative represented by the formula: ##STR1## wherein R is an alkyl group having 1 to 13 carbon atoms, A is a hydroxyl group or a group easily hydrolyzable to a hydroxyl group, X and Y together form an oxo group or an alkylenedioxy group having 2 or 3 carbon atoms, X is a hydroxyl group, an alkoxy group having 1 to 5 carbon atoms or a group easily hydrolyzable to a hydroxyl group, Y is a hydrogen atom or an alkoxy group having 1 to 5 carbon atoms, with the proviso that when X is a hydroxyl group or a group easily hydrolyzable to a hydroxyl group, Y is a hydrogen atom, and when X is an alkoxy group having 1 to 5 carbon atoms, Y is an alkoxy group having 1 to 5 carbon atoms, or a salt thereof.

REFERENCES:
patent: 5122521 (1992-06-01), Yamada
Tschesche, R. and Schwinum, E., "Synthese von 12.alpha..20R-Epoxy-5.alpha..14.beta..17.beta.H-pregnanen", Chem. Ber 100:464-479 (1967).
Elwood, et al, Biochemistry, 36(6), 1997, pp. 1467-1478.
Iguchi, et al: "Aragusterol A: A Potent Antitumor Marine Steroid from the Okinawan Sponge of the Genus", Xestospongia, Tetrahedron Letters, vol. 34, No. 39, pp. 6277-6280, 1993.
Tennen Yuki Kagobutsu Toronkai koen Yoshishu 35th,p. 274-281 (1993) Iguchi, et al:"Aragusterol A, B and C: potent antitumor marine steroids from the Okinawa sponge of the genis Xestospongia" (Chemical Abstracts 121:99238).

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