Synthesis and biological evaluation of novel carbazole-rhodanine conjugates as topoisomerase II inhibitors.

Basic Information

ID: ALA4184309

Journal: Bioorg Med Chem Lett

Title: Synthesis and biological evaluation of novel carbazole-rhodanine conjugates as topoisomerase II inhibitors.

Authors: Jiang H, Zhang WJ, Li PH, Wang J, Dong CZ, Zhang K, Chen HX, Du ZY.

Abstract: In this study, a series of carbazole-rhodanine conjugates was synthesized and evaluated for their Topoisomerase II inhibition potency as well as cytotoxicity against a panel of four human cancer cell lines. Among these thirteen compounds, 3a, 3b, 3g, and 3h possessed Topoisomerase II inhibition potency at 20 μM. Mechanism study revealed that these compounds may function as Topo II catalytic inhibitors. It was found that the electron-withdrawing groups on the phenyl ring of compounds played an important role on enhancing both enzyme inhibition and cytotoxicity.

CiteXplore: 29545100

DOI: 10.1016/j.bmcl.2018.03.017

Patent ID: