Аннотация:A design of molecules with effective anticancer properties constructed from both dually active metal complex and organic fragment is a novel trend in medicinal chemistry. This concept suggests impact of a drug on several biological targets or synergistically action both fragments as single unit. We propose that combination of Pd-metallocomplex fragment and organic unit can be interesting model for anticancer drug discovery. The first phase in development of such suggested molecules became synthesis of bilateral metallosystems, containing bioactive 6-substituted piperidin-2-one and palladated N-phenylpyrazolic fragment. Both fragments were incorporated into one molecule through the fused pyrazole-piperidine-2-one unit followed by pyrazol-directed cyclopalladation of phenyl-group with Pd(OAc)2. An effect of acceleration of the rate of the palladation by NH-lactame was observed. The synthesized hybrid palladacycles have been characterized and tested on cytotoxic activity on three cancerous cell lines as PPh3 complexes, revealing structures prospective for further development and structural optimization.