Synthesis and biological evaluation of a new class of triazin-triazoles as potential inhibitors of human farnesyltransferase

摘要

A new synthesis of ethynyldimethoxytriazine 1, an important platform-compound for developing new chemical entities for anticancer research and for other biological applications, is described. Compound 1 was further reacted with azides 5a-i to provide triazin-triazoles 2a-i, which were tested on human farnesyltransferase and on the NCI-60 human tumor cell lines. Synthesis of other dimethoxytriazine derivatives 15 and 16, linked to a sp (2) or a sp (3) carbon atom were also studied.