THE SYNTHESIS, ANTITUMOR ACTIVITY, AND SAR OF N-SUBSTITUTED γ-AMINOPROPYLSILATRANE DERIVATIVES

-Aminopropylsilatrane has been reported to possess biological activity against tumor cancer cells with low cytotoxicity in many kinds of silatranes. So some N-substituted -aminopropylsilatrane derivatives were synthesized and assayed by a primary anticancer screening against HT-29, Hela, and MDAMB435 cells by the use of the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) method. The structures of these derivatives were confirmed by H-1 NMR, electrospray ionization-mass spectrometry, and elemental analysis. The structure-activity relationship showed that the N-substituted derivatives exhibit better activity in which the -amino group of the silatrane is connected with stronger electron-withdrawing groups.