Medicinal Chemistry

Author(s): H. Cerecetto, M. Gonzalez, M. L. Lavaggi, M. A. Aravena, C. Rigol, C. Olea-Azar, A. Azqueta, A. Lopez de Cerain, A. Monge and A. M. Bruno

DOI: 10.2174/157340606778250207

Phenazine 5,10-Dioxide Derivatives as Hypoxic Selective Cytotoxins: Part II. Structure-Activity Relationship Studies

Page: [511 - 521] Pages: 11

  • * (Excluding Mailing and Handling)

Abstract

The synthesis and evaluation as hypoxic selective cytotoxins of new derivatives of 2-amino or 2- hydroxyphenazine 5,10-dioxide are described. The compounds were developed as structural analogs of other bioreductive compounds and its in vitro cytotoxicities on V79 cells under hypoxic and aerobic conditions were determined. To gain insight into its mechanism of action electrochemical behavior, interaction with DNA experiments and QSAR studies were performed.

Keywords: Phenazine 5, 10-dioxide derivatives, bioreductive compounds, DNA, cyclic voltammetry