Alkylthiocolchicines and N deacetyl alkylthiocolchicines and their antileukemic activity

Article abstract of DOI:10.1002/jps.2600640415

A series of alkylthiocolchicines (methyl, ethyl, n butyl, n hexyl, n octyl and pinanyl) was prepared from cholchicine by treatment with the appropriate alkyl mercaptan and p toluene sulfonic acid. Some of these compounds (methyl, ethyl, and n butylthiocolchicines) were deacetylated in good yields with 2 N hydrochloric acid in methanol. These compounds were tested for their antileukemic activity in an in vitro assay against L 1210 (mouse leukemia). Preliminary results showed that methylthiocolchicine is more active and the other alkylthiocolchicines are much less active than colchicine. N deacetyl methylthiocolchicine is as active as colchicine.