Novel rhodanine derivatives induce growth inhibition followed by apoptosis

✍ Scribed by Balaji T. Moorthy; Subban Ravi; Mrinal Srivastava; Kishore K. Chiruvella; H. Hemlal; Omana Joy; Sathees C. Raghavan

• Book ID: 104004807
• Publisher: Elsevier Science
• Year: 2010
• Tongue: English
• Weight: 914 KB
• Volume: 20
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.08.084

✦ Synopsis

We have designed and synthesized three novel compounds, 5-isopropylidiene derivatives of 3-dimethyl-2-thio-hydantoin (ITH-1), 3-ethyl-2-thio-2,4-oxazolidinedione (ITO-1), and 5-benzilidene-3-ethyl rhodanine (BTR-1), and have tested their chemotherapeutic properties. Our results showed that all three compounds induced cytotoxicity in a time- and concentration-dependent manner on leukemic cell line, CEM. Among the compounds tested, BTR-1 was 5- to 7-fold more potent than ITH-1 and ITO-1 when compared by trypan blue and MTT assays. IC(50) value of BTR-1 was estimated to be <10μM. Both cell cycle analysis and tritiated thymidine assays revealed that BTR-1 affects DNA replication by inducing a block at S phase. BTR-1 treatment led to increased level of ROS production and DNA strand breaks suggesting activation of apoptosis for induction of cell death.