 The purpose of this paper is to summarize mode of action of sysplatin on the tumor cells, a brief outlook on the metallocene compounds as antitumor drugs as well as the future tendencies for the use of the latter in anticancer chemotherapy. Molecular mechanisms of sysplatin interaction with DNA, DNA repair mechanisms, and cellular proteins are discussed. Molecular background of the sensitivity and resistance to sysplatin, as well as its influence on the efficacy of the antitumor immune response was evaluated. Furthermore, herein are summarized some metallocenes, titanocene, vanadocene, molybdocene, ferocene, and zirconocene, with high antitumor activity. This article was authored by Santiago Gomez-Ruiz, Daniella Maximovich Ivanovich, Sanja Mijatovic, and others.