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

Journal

MINI-REVIEWS IN MEDICINAL CHEMISTRY
Volume 9, Issue 12, Pages 1389-1396

Publisher

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/138955709789957422

Keywords

alpha-N-heterocyclic thiosemicarbazone; bis(thiosemicarbazone); ribonucleotide reductase inhibitors; antitumour agents; metal complexes; structure-activity relationships

Funding

  1. Ministerio de Ciencia e Innovacion
  2. Instituto de Salud Carlos III [PI040354, PI080525]
  3. Comunidad de Madrid [GR/SAL/0180/2004]
  4. Universidad Autonoma de Madrid-Comunidad de Madrid of Spain [CCG08-UAM/SAL-4000]

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alpha-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.

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