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Inhibition of Topoisomerase IIα by Metal Complexes of Selected Thiosemicarbazones
Author(s) -
Jiang Xiaohua,
Lisic Edward
Publication year - 2013
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.27.1_supplement.lb571
Subject(s) - topoisomerase , dna , dna replication , semicarbazone , chemistry , dna supercoil , cancer cell , apoptosis , cell growth , microbiology and biotechnology , biochemistry , biology , stereochemistry , cancer , genetics
Uncontrolled cell proliferation is the main characteristic of all cancer types. To kill the over‐proliferated cells is one key to cure cancer. Before cell proliferation, the genetic material, DNA, needs to be replicated. Thus, DNA replication is the top target for many anti‐cancer drugs. Topoisomerase IIα (Topo IIα) is essential for DNA replication in order to release the supercoiled DNA daughter strands produced after replication (topology simplification) and reduce entanglements. Topo IIα breaks DNA strands, which make it one of the most important targets for anticancer drugs since the accumulation of DNA nicks from inhibition of Topo IIα induces apoptosis. We have synthesized and characterized several structurally different series of thiosemicarbazone ligands and their metal complexes, which show different inhibition activities towards Topo IIα. Our studies indicate that several of the new compounds exhibit high Topo IIα inhibition and are potential anticancer drugs.