Bile acid derivatives, their salts and production thereof

Details Bile acid derivatives, their salts and production thereof Bile acid derivatives, their salts and production thereof

1987-09-01

1989-03-07

Schenkman, Leonard

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

C07J 100

Patent

active

048104221

ABSTRACT:
A bile acid derivative of the following formula (I): ##STR1## wherein: X is a halogen atom; R.sub.1 is a hydrogen atom or a lower alkyl group; Y is ##STR2## (wherein n is an integer of from 0 to 5); each of R.sub.2 and R.sub.3 is a hydrogen atom or a hydroxyl group; R.sub.4 is a hydroxyl group, lower alkoxyl group, ##STR3## (wherein R.sub.5 is a hydrogen atom or a lower alkoxy group, R.sub.6 is a carboxyl group, benzyloxycarbonyl group or sulfonyl group, or a salt thereof, and m is an integer of from 1 to 4); the intermittent line, . . . , is an .alpha.-bond; and the wavy line, , is an .alpha.- or .beta.-bond, and a salt thereof, and a process for production thereof.
This bile acid derivative has carcinostatic activity and yet is of low toxicity. Accordingly, this compound can be used as a carcinostatic agent.

REFERENCES:
Carroll et al., Journal of Medicinal Chemistry, 1972, 15 (11), pp. 1158-1161.
Niculescu-Duvaz et al., J. Prakt. Chem., 1979, 321 (3), pp. 522-528.
Wolf et al., J. Org. Chem., 1973, 38 (7), pp. 1276-1279.
Baracu et al., Rev. Roum. Chim., 1985, 30 (4), pp. 317-327.
Chemical Abstracts; vol. 103, (1985), #134470g; Baracu et al.
Chemical Abstracts; vol. 98, (1983), #179757a; Niculescu-Duvaz et al.
Chemical Abstracts; vol. 91, (1979), #211670k; Niculescu-Duvaz et al.
Chemical Abstracts; vol. 79, (1973), #136513n; Wolf et al.

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