Design, synthesis and biological evaluation of lapachol derivatives possessing indole scaffolds as topoisomerase I inhibitors
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- 作者：Chong Zhanga ; zhangchong2006@163.com" class="auth_mail" title="E-mail the corresponding author ; Yan Qub ; Bingxuan Niua
- 关键词：WVWZDUZSNYDZHH-UHFFFAOYSA-N ; WNVLVESSJIQBDA-UHFFFAOYSA-N ; OIPVNVUYHWFWKU-UHFFFAOYSA-N ; CHKHITCFNJDQBB-UHFFFAOYSA-N ; ZTJOAMULLFTRLP-UHFFFAOYSA-N ; NNXPCSUYLLFIMP-UHFFFAOYSA-N ; HMOCMMSHXMENBG-UHFFFAOYSA-N ; PDRHPQXIVFDWOC-UHFFFAOYSA-N ; GNJJTVWRDDUQJF-UHFFFAOYSA-N ; KOCCJLZMVZIWJK-UHFFFAOYSA-N ; YBIUQXNNKWZOGM-UHFFFAOYSA-N ; MAUZANVZGIYTBC-UHFFFAOYSA-N ; GLVWVFNCPKPIBR-UHFFFAOYSA-N ; CWAXYBQQTIOGRI-UHFFFAOYSA-N ; GCPIOKVXWZZEOQ-UHFFFAOYSA-N ; CIEYTVIYYGTCCI-UHFFFAOYSA-N
- 刊名：Bioorganic & Medicinal Chemistry
- 出版年：2016
- 出版时间：15 November 2016
- 年：2016
- 卷：24
- 期：22
- 页码：5781-5786
- 全文大小：972 K
文摘
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A series of novel lapachol derivatives fused indoles was designed and synthesized.
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Anti-proliferative activity was assessed against Eca109 and Hela cell lines.
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The novel compounds have potent Topo I inhibition activity.
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The novel compounds can induce Hela cell apoptosis.