Mini-Reviews in Medicinal Chemistry

Author(s): Ana I. Matesanz and Pilar Souza

DOI: 10.2174/138955709789957422

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α-N-Heterocyclic Thiosemicarbazone Derivatives as Potential Antitumor Agents: A Structure-Activity Relationships Approach

Page: [1389 - 1396] Pages: 8

  • * (Excluding Mailing and Handling)

Abstract

α-N-Heterocyclic thiosemicarbazones, (N)-TSCs, are potent inhibitors of ribonucleotide reductase (RR). This enzyme plays a critical role in DNA synthesis and repair, and is a well-recognized target for cancer chemotherapeutic agents. In this review the structural features of (N)-TSCs, required for maximum antitumour activity have been explored. Special attention is given to the mechanisms of action and structure-activity relationships.

Keywords: α-N-heterocyclic thiosemicarbazone, bis(thiosemicarbazone), ribonucleotide reductase inhibitors, antitumour agents, metal complexes, structure-activity relationships