Selenium-containing naphthalimides as anticancer agents: Design, synthesis and bioactivity

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• 作者：Liwei Zhao^a ; ^b ; Jianfeng Li^a ; Yiquan Li^a ; Jianwen Liu^a ; Thomas Wirth^b ; Zhong Li^a ; ^{lizhong@ecust.edu.cn}
• 关键词：HAJMPZOOPNLYMA-UHFFFAOYSA-N ; ANHKQOODXXPXDS-UHFFFAOYSA-N ; FZVXIPMUWUEMLU-UHFFFAOYSA-N ; WCSDPIZCMBOSNF-UHFFFAOYSA-N ; ZDLCMDOEDUHSML-UHFFFAOYSA-N ; WJPZPGLTIHFMSA-UHFFFAOYSA-N ; SOBWJWVTKILDGU-UHFFFAOYSA-N ; GLKSQUYGECERLH-UHFFFAOYSA-N
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2012
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：15 April, 2012
• 卷：20
• 期：8
• 页码：2558-2563
• 文件大小：691 K

摘要

Selenium analogues (4b-4h, and 4j) of two known sulfur compounds were synthesized and tested their anticancer activities. The selenium compound 4b had comparable activity with its sulfur analogue 4a, while DNA-binding study showed these two compounds had similar interaction with ct-DNA, the K_b was 8.23 and 2.36, respectively. The primary results showed that most compounds had moderate anticancer activities with IC₅₀ values between 10^鈭? and 10^鈭? M. Another selenium analogue 4j showed the highest activity with the IC₅₀ values around 5.3 渭M against K562 and MCF-7 cell lines. More importantly, the organochalcogen compounds exhibited stronger anticancer activities against K562 cell line than the other cell lines tested.