Intoplicine (RP 60475) and its derivatives, a new class of antitumor agents inhibiting both topoisomerase I and II activities.

@article{Riou1993Intoplicine6,
  title={Intoplicine (RP 60475) and its derivatives, a new class of antitumor agents inhibiting both topoisomerase I and II activities.},
  author={Jean François Riou and P. Fosse and Chi Hung Nguyen and Annette K. Larsen and Marie Christine Bissery and L Grondard and Jenifer M Saucier and Emile Bisagni and François Lavelle},
  journal={Cancer research},
  year={1993},
  volume={53 24},
  pages={5987-93}
}
Intoplicine (RP 60475, NSC 645008) is an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series which is now being tested in clinical trials. Intoplicine strongly binds DNA (KA = 2 x 10(5) M-1) and thereby increases the length of linear DNA. These properties are consistent with DNA unwinding by intoplicine. Intoplicine was found to be a dual topoisomerase I and II inhibitor, with DNA sites of enzyme inhibition being different for these two enzymes. In this study, 22 analogues of… CONTINUE READING

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DNA Topoisomerases in Cancer Therapy

DN A Topoisomerases, Toshiwo Andoh
Springer US • 2003

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