Moorthy, Balaji T. ; Ravi, Subban ; Srivastava, Mrinal ; Chiruvella, Kishore K. ; Hemlal, H. ; Joy, Omana ; Raghavan, Sathees C. (2010) Novel rhodanine derivatives induce growth inhibition followed by apoptosis Bioorganic & Medicinal Chemistry Letters, 20 (21). pp. 6297-6301. ISSN 0960-894X
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Official URL: http://www.sciencedirect.com/science/article/pii/S...
Related 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 μM. 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.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Elsevier Science. |
| Keywords: | Chemotherapy; Double-strand Breaks; Cytotoxicity; DNA Damage; 5-Benzilidene-3-ethyl Rhodanine |
| ID Code: | 103938 |
| Deposited On: | 04 Apr 2017 09:52 |
| Last Modified: | 04 Apr 2017 09:52 |
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