Abstract: Antitumor compounds based on the ?1-adrenoceptor antagonist, doxazosin, as well as compositions and methods of use. The disclosed compounds induce apoptosis in cancer cells.

Abstract: Provided is a method of inhibiting the growth of prostate cancer cells comprising administering an effective amount of DZ-50 (2-[4-biphenyl-4-sulfonyl)-piperazin-1-yl]-6,7-diisopropoxyquinazolin-4-yl-amine) to a patient in need thereof. In another aspect, a method is provided for inhibiting the initiation of prostate cancer comprising administering an effective amount of DZ-50 to a patient in need thereof. In yet another aspect, a method is provided for inhibiting the formation of a prostate tumor-derived metastatic lesion comprising administering an effective amount of DZ-50 to a patient in need thereof. In any of the aforementioned methods, a quinazoline-based drug which induces apoptosis of a prostate cancer cell may be coadministered with DZ-50. Also provided is a composition comprising DZ-50, a quinazoline-based drug which induces apoptosis of a prostate cancer cell, and a pharmaceutically acceptable carrier.