New agents for prostatic cancer activated specifically by prostatic acid phosphatase.

Potential cytotoxic compounds (spindle poisons) are being designed for the treatment of prostatic carcinoma, using the structural requirements of the substrates for prostatic acid phosphatase (PAP). Colchicine has been modified in ring C to give colchiceinamides of substituted ethanolamines and ethanolaminephosphates. Another new series of compounds modifying ring B of thiocolchicine have been prepared. Three O-phosphates of the thiocolchicine series have also been made. One has been examined for its specificity toward PAP. Some toxicity data of these compounds in mice have also been reported. Colchiceinamide-(L)-ephedrinephosphate has been examined in stumptail monkeys and some preliminary results are reported here.