Résumé : Pd(II) complexes with organophosphines and dithiocarbamates derivatives of α-amino acids were synthesized by reacting N,N-dicyclohexyldithiocarbamate (DCHDTC, compounds 1–3) and N-methylcyclohexyldithiocarbamate (MCHDTC, compounds 4–6) with (R3P)2PdCl2 (R = Ph, o-tolyl, Ph2Cl) in a 1:1 molar ratio. The complexes were characterized by elemental analyses, FT-IR, multinuclear (1H, 13C and 31P) NMR and single X-ray crystallography, showing that the dithiocarbamate acts as a bidentate ligand and binds to Pd(II) via two sulfur atoms, resulting in a square planar geometry around Pd(II). The cytotoxicity of compounds 2, 3 and 4 was determined in vitro against six human tumour cell lines, MCF7, EVSA-T, WIDR, IGROV, M19 MEL, A498 and H226. Compounds 3 and 4 showed a moderate to low cytotoxicity, whereas compound 2 exhibited a very low cytotoxicity. The results of antifungal assays showed that compounds 1–6 possess antifungal activity against Fusarium moniliformes, Fusarium saolani, Mucor sp., Aspergillus niger and Aspergillus fumigatus. The anti-inflammatory screening results of 1–6 are quite similar to those observed for the standard drug Declofenac at 10 mg kg−1, which inhibited the odema by 74% after 4 h. Copyright © 2007 John Wiley & Sons, Ltd.