Background:

Intoplicine is a DNA topoisomerase I and II inhibitor.

Activity of Intoplicine (RP60475), a new DNA topoisomerase I and II inhibitor, against human tumor colony-forming units in vitro. Intoplicine (RP60475) is the most active analogue evaluated in the 7H-benzo[e]-pyrido-[4,3-b]-indole series of antineoplastic compounds. Intoplicine exerts its activity through inhibition of DNA topoisomerase I and II[1]. Intoplicine is found to unwind DNA and to inhibit purified calf thymus topoisomerase II via a stabilization of the ternary cleavable complex[2].

[1]. Eckardt JR, et al. Activity of Intoplicine (RP60475), a new DNA topoisomerase I and II inhibitor, against human tumor colony-forming units in vitro. J Natl Cancer Inst. 1994 Jan 5;86(1):30-3. [2]. Morjani H, et al. Molecular and cellular interactions between Intoplicine, DNA, and topoisomerase II studied by surface-enhanced Raman scattering spectroscopy. Cancer Res. 1993 Oct 15;53(20):4784-90.