A new synthesis of ethynyldimethoxytriazine 1, an important platformcompound 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. Electronic supplementary material The online version of this article (2a-i target compounds CO 2 H 2c: IC 50 (human FTase) = 38.6 µM