Moorthy, Balaji T and Ravi, Subban and Srivastava, Mrinal and Chiruvella, Kishore K. and Hemlal, H. and Joy, Omana and Raghavan, Sathees C (2010) Novel rhodanine derivatives induce growth inhibition followed by apoptosis. In: Bioorganic & Medicinal Chemistry Letters, 20 (21). pp. 6297-6301.
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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. IC50 value of BTR-1 was estimated to be <10 mu M. 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. (C) 2010 Elsevier Ltd. All rights reserved.
|Item Type:||Journal Article|
|Additional Information:||Copyright of this article belongs to Elsevier Science.|
|Keywords:||Chemotherapy; Double-strand breaks; Cytotoxicity; DNA damage; 5-Benzilidene-3-ethyl rhodanine.|
|Department/Centre:||Division of Biological Sciences > Biochemistry|
|Date Deposited:||28 Oct 2010 06:21|
|Last Modified:||28 Oct 2010 06:21|
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