Abstract: The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.

Abstract: Compounds according to formula I: C′—L—T (I), wherein C′ is a camptothecin group; L is a linking moiety; T is a taxoid group, pharmaceutically acceptable salt thereof. The compounds are useful in, among other things, treating cancer in subjects in need thereof, including cellular differentiation, and inhibiting cellular mitosis.