1. Academic Validation
  2. Selenium-containing naphthalimides as anticancer agents: design, synthesis and bioactivity

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

  • Bioorg Med Chem. 2012 Apr 15;20(8):2558-63. doi: 10.1016/j.bmc.2012.02.049.
Liwei Zhao 1 Jianfeng Li Yiquan Li Jianwen Liu Thomas Wirth Zhong Li
Affiliations

Affiliation

  • 1 Shanghai Key Lab of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Meilong Road 130, Shanghai 200237, China.
Abstract

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 IC(50) values between 10(-6) and 10(-5) M. Another selenium analogue 4j showed the highest activity with the IC(50) 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.

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