Acridine derivatives as inhibitors/poisons of topoisomerase II

Synthesis and antiproliferative activity of 9-benzylamino-6-chloro-2-methoxy-acridine derivatives as potent DNA-binding ligands and topoisomerase II inhibitors

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2016.03.066 ◽

2016 ◽

Vol 116 ◽

pp. 59-70 ◽

Cited By ~ 25

Author(s):

Wei Zhang ◽

Bin Zhang ◽

Wei Zhang ◽

Ti Yang ◽

Ning Wang ◽

...

Keyword(s):

Dna Binding ◽

Antiproliferative Activity ◽

Topoisomerase Ii ◽

Acridine Derivatives ◽

Topoisomerase Ii Inhibitors

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Novel tetra-acridine derivatives as dual inhibitors of topoisomerase II and the human proteasome

Biochemical Pharmacology ◽

10.1016/j.bcp.2007.02.016 ◽

2007 ◽

Vol 73 (12) ◽

pp. 1863-1872 ◽

Cited By ~ 35

Author(s):

S. Vispé ◽

I. Vandenberghe ◽

M. Robin ◽

J.P. Annereau ◽

L. Créancier ◽

...

Keyword(s):

Topoisomerase Ii ◽

Acridine Derivatives ◽

Dual Inhibitors

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The in vivo distribution and dynamics of DNA topoisomerase II in Drosophila embryonic nuclei and chromosomes

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100146217 ◽

1993 ◽

Vol 51 ◽

pp. 74-75

Author(s):

Jason R. Swedlow ◽

Neil Osheroff ◽

Tim Karr ◽

John W. Sedat ◽

David A. Agard

Keyword(s):

Topoisomerase Ii ◽

Biochemical Characterization ◽

Developmental Cycle ◽

Dna Topoisomerase Ii ◽

Chromosomal Distribution ◽

Dna Topoisomerase ◽

Ideal System ◽

Dnase Treatment

DNA topoisomerase II is an ATP-dependent double-stranded DNA strand-passing enzyme that is necessary for full condensation of chromosomes and for complete segregation of sister chromatids at mitosis in vivo and in vitro. Biochemical characterization of chromosomes or nuclei after extraction with high-salt or detergents and DNAse treatment showed that topoisomerase II was a major component of this remnant, termed the chromosome scaffold. The scaffold has been hypothesized to be the structural backbone of the chromosome, so the localization of topoisomerase II to die scaffold suggested that the enzyme might play a structural role in the chromosome. However, topoisomerase II has not been studied in nuclei or chromosomes in vivo. We have monitored the chromosomal distribution of topoisomerase II in vivo during mitosis in the Drosophila embryo. This embryo forms a multi-nucleated syncytial blastoderm early in its developmental cycle. During this time, the embryonic nuclei synchronously progress through 13 mitotic cycles, so this is an ideal system to follow nuclear and chromosomal dynamics.

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