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The study of the reactivity of the pyrazole derivative 1‐[MeO(CH2)2]‐3,5‐Ph2‐4‐(CH2Fc)–(C3N2) (1, Fc = ferrocenyl) with Na2[PdCl4], Pd(OAc)2, and [MCl2(dmso)2] (M = Pd or Pt, dmso = dimethyl sulfoxide) has allowed us to isolate trans‐[Pd{κ‐N‐(1‐{MeO(CH2)2}‐3,5‐Ph2‐4‐{CH2Fc}–{C3N2})}2Cl2] (2), [Pd{κ2‐C,N(1‐{MeO(CH2)2}‐3‐{C6H4}‐5‐Ph‐{C3N2})}{κ‐N‐(1‐{MeO(CH2)2}‐3,5‐Ph2‐4‐{CH2Fc}–{C3N2})}Cl] (3), [Pd{κ2‐C,N(1‐{MeO(CH2)2}‐3‐{C6H4}‐4‐{CH2Fc}‐5‐Ph‐{C3N2})}Cl(PPh3)] (4), and the trans (5) and cis (6) isomers of [Pt{κ‐N‐(1‐{MeO(CH2)2}‐3,5‐Ph2‐4‐{CH2Fc}–{C3N2})}Cl2(dmso)]. Compound 1 acts as a N (in 2, 5, and 6) or (C,N)– donor ligand (in 4) and shows both binding modes in 3. The cytotoxic assessment of 1–6 against MCF7, MDA‐MB231 (breast), and HCT‐116 (colon) cancer cell lines reveal that (1) 1 is more potent than 1‐[MeO(CH2)2]‐3,5‐Ph2‐(C3HN2) (V), (2) 2–6 have cytotoxic activity, (3) 2 and 3 are less active than 4–6, and (4) 6 is the most potent compound against the three cancer cell lines.