Estradiol derivative-chlorambucil conjugate process for preparin

Details Estradiol derivative-chlorambucil conjugate process for preparin Estradiol derivative-chlorambucil conjugate process for preparin

1993-06-03

1994-10-11

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

514179, 514180, 514182, 552613, 552614, 552615, 552617, 552618, 552626, C07J 100

Patent

active

053547454

ABSTRACT:
An estradiol derivative-chlorambucil conjugate of the formula (I): ##STR1## wherein R.sup.1 is alkyl or alkoxyl of 1 to 4 carbon atoms; R.sup.2 is acyl, dansyl, or alkyl; R.sup.3, R.sup.4, and R.sup.5 independently are H, oxo, OH, or acyloxy; m is an integer of 1 to 3; and n is an integer of 0 to 3; provided that when n is 0, all of R.sup.3, R.sup.4, and R.sup.5 are not H at the same time, and at least one of R.sup.3, R.sup.4, and R.sup.5 is a group other than H and OH; and further, when n is 2 or 3, the groups R.sup.1 are the same or different; a process for preparing the same, and a pharmaceutical composition containing the conjugate are described.

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Anticancer Research, Kubota, et al., vol. 13 pp. 935-940 (1993).
Kosano, et al., Cancer Research, vol. 52, pp. 1187-1191 (1992).

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