Synthesis, Antitumor Activity, and SAR of N-Substituted γ-Aminopropylsilatrane Derivatives

Abstract

γ-Aminopropylsilatrane has been reported to possess biological activity against tumor cancer cells with low cytotoxicity in many kinds of silatranes. So some N-substituted γ-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 ¹H NMR, electrospray ionization-mass spectrometry, and elemental analysis. The structure–activity relationship showed that the N-substituted derivatives exhibit better activity in which the γ-amino group of the silatrane is connected with stronger electron-withdrawing groups.

GRAPHICAL ABSTRACT

Keywords:

• γ-Aminopropylsilatrane derivatives
• structure–activity relationship (SAR)
• physiological activity