Mitotic arrest induced by a novel family of DNA topoisomerase II inhibitors.
Basic Information
ID: ALA1157743
Journal: J Med Chem
Title: Mitotic arrest induced by a novel family of DNA topoisomerase II inhibitors.
Authors: León LG, Ríos-Luci C, Tejedor D, Pérez-Roth E, Montero JC, Pandiella A, García-Tellado F, Padrón JM.
Abstract: A small structure-focused library of propargylic enol ethers was prepared by means of a modular and efficient chemodifferentiating organocatalyzed multicomponent reaction. The most active compound (GI(50) 0.25 microM) against solid tumor cells was selected as lead. Cell cycle analysis and immunoblotting demonstrated arrest at the metaphase, pointing out human topoisomerase II as plausible molecular target. In vitro assays were carried out, showing that the lead behaves as a catalytic inhibitor of the enzyme.
CiteXplore: 20405921
DOI: 10.1021/jm100155y
Patent ID: ┄