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

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 (6) and 10 (5) M. Another selenium analogue 4j showed the highest activity with the IC50 values around 5.3 mu 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. Crown Copyright (C) 2012 Published by Elsevier Ltd. All rights reserved.