Alkylthiocolchicines and N-deacetyl-alkylthiocolchicines and their antileukemic activity.

Autor: Shiau GT, De KK, Harmon RE
Jazyk: angličtina
Zdroj: Journal of pharmaceutical sciences [J Pharm Sci] 1975 Apr; Vol. 64 (4), pp. 646-8.
DOI: 10.1002/jps.2600640415
Abstrakt: A series of alkylthiocolchcines (methyl, ethyl, n-butyl, n-hexy, n-octyl, and pinanyl) was prepared from colchicine by treatment with the appropriate alkyl mercaptan and p-toluenesulfonic 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.
Databáze: MEDLINE