2. Academic Validation
  3. Design, synthesis and biological evaluation of lapachol derivatives possessing indole scaffolds as topoisomerase I inhibitors

Design, synthesis and biological evaluation of lapachol derivatives possessing indole scaffolds as topoisomerase I inhibitors

  • Bioorg Med Chem. 2016 Nov 15;24(22):5781-5786. doi: 10.1016/j.bmc.2016.09.034.
Chong Zhang 1,  Yan Qu 2,  Bingxuan Niu 3
Affiliations

Affiliations

  • 1 School of Pharmacy, Xinxiang Medical University, Xinxiang 453003, China. Electronic address: zhangchong2006@163.com.
  • 2 Basic Medicine College, Xinxiang Medical University, Xinxiang 453003, China.
  • 3 School of Pharmacy, Xinxiang Medical University, Xinxiang 453003, China.
PMID: 27667553 DOI: 10.1016/j.bmc.2016.09.034
Abstract

A series of novel lapachol derivatives possessing indole scaffolds was designed and synthesized. The in vitro anti-proliferative activity of these novel compounds was evaluated in Eca109 and Hela cell lines. Almost all the tested compounds showed manifested potent inhibitory activity against the two tested Cancer cell lines. Topo I-mediated DNA relaxation activity indicated that these novel compounds have potent Topoisomerase I inhibition activity. The most potent compounds 4n and 4k demonstrated more cytotoxicity than camptothecin and was comparable to camptothecin in inhibitory activities on Topoisomerase I in our biological assay. In addition, the Hoechst 33342 staining method also showed that the complex can induce Hela cell Apoptosis.

Keywords

Anti-proliferative; Indole; Lapachol; Molecular hybridization; Topoisomerase I.

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