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Novel rhodanine derivatives induce growth inhibition followed by apoptosis

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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Official URL: http://dx.doi.org/10.1016/j.bmcl.2010.08.084

Abstract

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
URI: http://eprints.iisc.ernet.in/id/eprint/33451

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