Synthesis and bioactivities of steroid derivatives as antifungal agents

A series of lanosterol and cholesterol derivatives with modified side chain structures, which might interfere with sterol C24-methyltransferase in the ergosterol biosynthesis as substrate analogs, have been synthesized. The i n vitro bioassay studies have shown that some of these compounds, in partic ular with C24-amino- and thio-functionalities, possess potent antifungal ac tivities. in vivo. Bioassays have also been carried out for the leading com pounds. (C) 1998 Elsevier Science Ltd. All rights reserved.