NOVEL ESTRADIOL DERIVATIVE-CHLORAMBUCIL CONJUGATE, PROCESS FOR PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITION

摘要

An estradiol derivative-chlorambucil conjugate of the formula (II) IMG (II) wherein R1 is alkyl or alkoxyl of 1 to 4 carbon atoms; R2 is acyl, dansyl, or alkyl; R3, R4, and R5 independently are H, oxo, OH, or acyloxy; m is an integer of 1 to 3; n is an integer of 0 to 3; and X is halogen, OH, or a salt thereof; provided that when n is 0, all of R3, R4, and R5 are not H at the same time, and at least one of R3, R4, and R5 is a group other than H and OH; and further, when n is 2 or 3, the groups R1 are the same or different; a process for preparing the same, and a pharmaceutical composition containing the conjugate are described.