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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

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

doi

10.1016/j.bmcl.2018.03.017

subject

Has Abstract

pub_date

2018-05-01 00:00:00

pages

1320-1323

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(18)30196-3

journal_volume

28

pub_type

杂志文章

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