Synthesis and Bioactivity Evaluation of Acylthiourea Derivatives Based on Isopimaric Acid

To develop isopimaric acid derivatives with high bioactivity, fifteen acyl (amide) thiourea derivatives containing isopimaric acid skeleton were synthesized and confirmed by FT-IR, H-1 NMR, C-13 NMR and HRMS or elemental analysis. All the compounds were evaluated for their antibacterial and anticancer activity. Most of the compounds showed siginificant inhibitory activity which was higher than that of isopiamric acid against the Candida Albicans. At the concentration of 100 mu mol/L, many compounds exhibited pronounced inhibitory effects on human melanoma cells (A375) and prostatic carcinoma (PC-3) cell lines, especially compounds N-isopimaric acyl-N'-(3-methylphenyl) sulfourea (3c) and N-isopimaric acylamino-N'-(4-fluorophenyl) sulfourea (6b) have the best anticancer activity, both with the inhibitory rate of over 90%.