In this study, we investigated the anticancer properties of methoxy-substituted nickel(II)(salophene) derivatives. We demonstrated that the most active complex [NiII(3-OMe-salophene)] is not necrotic in Burkitt-like lymphoma cells (BJAB) and human B-cell precursor cells (Nalm-6). [NiII(3-OMe-salophene)] inhibited proliferation and induced apoptosis in a concentration dependent manner, giving evidence for the involvement of CD95 receptor-mediated, extrinsic pathway. Furthermore, [NiII(3-OMe-salophene)] overcame vincristine drug resistance in BJAB and Nalm-6 cells.

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HUNI 068 is a promising new compound with activity even against MDR tumor cells. Further investigations into the class of ferrocene-derived agents might reveal compounds with improved activity for a more specific and safe anti-cancer therapy.

As previous studies in the field of bioorganometallic chemistry have unveiled, metal‐containing analogues of natural products frequently exhibit surprising biological activities. In this context, a synthetic approach to analogues of the eicosanoids 5‐HETE and 8‐HETE possessing a 1,3‐butadiene–Fe(CO)3 substructure was elaborated. The chosen structures are characterized by a central (2E,4Z)‐hexa‐2,4‐dien‐1‐ol–Fe(CO)3 moiety (as the potential “metal pharmacophore”) and carry a lipophilic ω‐6‐substituent as well as a hydrophilic α‐side chain (carboxylic acid). Using the cationic complex tricarbonyl[η5‐1‐(methoxycarbonyl)pentadienyl]iron hexafluorophosphate (rac‐4) as a starting material, the synthesis of a simplified Fe(CO)3‐complexed HETE analogue (rac‐3) was achieved by exploiting the addition of an alkynyl Cu species to rac‐4. The carbon skeleton was completed through diastereo(Ψ‐exo)selective addition of a titanium–zinc organyl [prepared from ethyl 4‐iodobutyrate, activated Zn powder, and Ti(OiPr)3Cl] as a butyrate D4 synthon to an aldehyde function by using 2‐Me‐THF as the solvent of choice. The (sensitive) target compound rac‐3 was shown to induce apoptosis at moderate concentrations in cancer cells (BJAB and Nalm‐6).