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

Zhao, Liwei, Li, Jianfeng, Li, Yiquan, Liu, Jianwen, Wirth, Thomas and Li, Zhong 2012. Selenium-containing naphthalimides as anticancer agents: Design, synthesis and bioactivity. Bioorganic and Medicinal Chemistry 20 (8) , pp. 2558-2563. 10.1016/j.bmc.2012.02.049

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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 Kb was 8.23 and 2.36, respectively. The primary results showed that most compounds had moderate anticancer activities with IC50 values between 10−6 and 10−5 M. Another selenium analogue 4j showed the highest activity with the IC50 values around 5.3 μM 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.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Subjects: Q Science > QD Chemistry
R Medicine > R Medicine (General)
Uncontrolled Keywords: Anticancer; Naphthalimides; Selenium; K562; DNA
Publisher: Elsevier
ISSN: 0968-0896
Last Modified: 04 Jun 2017 03:46

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