Synthesis and biological evaluation of peptidomimetics containing the tryptamine moiety as a potential antitumor agent

Abstract

Three series of novel peptidomimetics bearing the tryptamine moiety were designed, synthesized, and evaluated for their inhibition activities against cell proliferation. According to the preliminary studies on cytotoxic activities, some of the newly prepared compounds (Ia–k, IIa–d, IIIa–g) displayed significant inhibition activities against human hepatoma cancer (HepG2 and Huh-7), and human melanoma (A875) cell lines compared with the control 5-fluorouracil. Especially, compounds Ih and Ij exhibited obvious inhibition activities (Ih IC₅₀ = 4.88 ± 0.78 μg mL⁻¹; Ij IC₅₀ = 6.60 ± 1.20 μg mL⁻¹) against 5-fluorouracil-resistant human hepatocellular carcinoma (BEL-7402/5-FU) cell lines.