Basappa and Ananda Kumar, C. S. and Nanjunda Swamy, S. and Sugahara, Kazuyuki and Rangappa, K. S. (2009) Anti-tumor and anti-angiogenic activity of novel hydantoin derivatives: inhibition of VEGF secretion in liver metastatic osteosarcoma cells. Bioorganic & Medicinal Chemistry, 17 (14). pp. 4928-4934. ISSN 1464-3391
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A series of new azaspiro bicyclic hydantoin derivatives has been designed and synthesized. Initially, the anti-proliferative effect of the hydantoin derivatives was evaluated against human ovarian cancer cells (SKOV-3 and OVSAHO) and murine osteosarcoma cells (LM8 and LM8G7). Among the tested compounds, 8-(3-fluorobenzyl)-1'-(4-(methylsulfonyl)benzyl)-8-azaspirobicyclo 3.2.1]octane-3,4'-imidazolidine]-2',5'-dione (7h) and 8-(3,4-difluorobenzyl)-1'-(4-(methylsulfonyl)benzyl)-8-azaspirobicycl o3.2.1]octane-3,4'- imidazolidine]-2',5'-dione (7i) showed a significant anti-proliferative activity against the OVSAHO and LM8G7cells. The real-time monitoring of the effect of the compounds7h and 7i against the proliferation of LM8G7 was revealed that resulting IC50 values were 102 mu M and 13 mu M, respectively. We reasoned that the presence of fluorine atom at the 3rd position of the phenyl ring of the hydantoin side chain may determine the potency of the molecule. Furthermore, the compound 7i inhibited the tube formation of the mouse endothelial cells. Finally, the treatment of the compound 7i against the proliferation of LM8G7 cells demonstrated the down regulation of the secretion of VEGF, indicate the potential angioinhibitory effects. In conclusion, our findings demonstrate the suppression of the secretion of VEGF by LM8G7 cells by the compound 7i might contribute at least in part to the antitumor action. (C) 2009 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | Anti-tumor; Hydantoin; Anti-angiogenesis; VEGF; Metastasis |
| Subjects: | C Chemical Science > Chemistry |
| Divisions: | Department of > Chemistry |
| Depositing User: | Users 19 not found. |
| Date Deposited: | 22 Aug 2019 05:40 |
| Last Modified: | 22 Aug 2019 05:40 |
| URI: | http://eprints.uni-mysore.ac.in/id/eprint/6873 |
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