Abstract
Design and synthesis of a new class of potent hybrid compounds obtained by joining NO-donor furoxanyl moieties, through an appropriate spacer arm, to the pemetrexed segment, which was prepared in a modified simple route, are presented. Structures of all the target compounds were characterized by using Fourier-transform infrared (FT-IR), 1H-nuclear magnetic resonance (NMR), 13C-NMR, and electrospray ionization mass spectroscopy (ESI-MS). In addition, preliminary evaluation of antitumor activity using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) assay based on four different cancer cell lines (BGC-1, HL60-1, SMMC-1, and A549-1) was performed. The results suggested that different length of spacer arm in the hybrid compounds did have an impact on the molecules’ capability to inhibit cancer cell growth to various degrees, but without showing significant difference on regular pharmacological behaviors. Among all the synthesized hybrids, compound 1f showed the strongest inhibitory activity against all the tested cell lines and it is currently under our further investigation.
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