2. Academic Validation
  3. Synthesis and biological evaluation of novel carbazole-rhodanine conjugates as topoisomerase II inhibitors

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

  • Bioorg Med Chem Lett. 2018 May 1;28(8):1320-1323. doi: 10.1016/j.bmcl.2018.03.017.
Hong Jiang 1,  Wen-Jin Zhang 1,  Peng-Hui Li 2,  Jian Wang 3,  Chang-Zhi Dong 4,  Kun Zhang 5,  Hui-Xiong Chen 6,  Zhi-Yun Du 7
Affiliations

Affiliations

  • 1 Institute of Natural Medicine & Green Chemistry, School of Chemical Engineering and Light Industry, Guandong University of Technology, Guangzhou 510006, China.
  • 2 Institute of Natural Medicine & Green Chemistry, School of Chemical Engineering and Light Industry, Guandong University of Technology, Guangzhou 510006, China. Electronic address: liphsiming@163.com.
  • 3 School of Pharmaceutical Sciences, Tsinghua University, Beijing 100084, China.
  • 4 Institute of Natural Medicine & Green Chemistry, School of Chemical Engineering and Light Industry, Guandong University of Technology, Guangzhou 510006, China; Universite Paris Diderot, Sorbonne Paris Cite, ITODYS, UMR 7086 CNRS, 15 rue J-A de Baif, 75270 Cedex 13 Pairs, France.
  • 5 Institute of Natural Medicine & Green Chemistry, School of Chemical Engineering and Light Industry, Guandong University of Technology, Guangzhou 510006, China; Wuyi University, Jiangmen 529020, China.
  • 6 Institute of Natural Medicine & Green Chemistry, School of Chemical Engineering and Light Industry, Guandong University of Technology, Guangzhou 510006, China; CNRS, UMR8601, Laboratoire de Chimine et Biochimie Pharmacologiques et Toxicologiques, CBNIT, Universite Paris Descartes PRES Sorbonne Paris Cite, UFR Bio5medicale, 45 rue des Saints-Peres, 75270 Paris Cedex 06, France.
  • 7 Institute of Natural Medicine & Green Chemistry, School of Chemical Engineering and Light Industry, Guandong University of Technology, Guangzhou 510006, China. Electronic address: zhiyundu@gdut.edu.cn.
PMID: 29545100 DOI: 10.1016/j.bmcl.2018.03.017
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.

Keywords

Carbazole; Cytotoxic; Hybrid molecule; Rhodanine; Topoisomerase II.

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