Thimmegowda, N. R. and Kavitha, C. V. and Chiruvella, Kishore K. and Joy, Omana and Rangappa, K. S. and Raghavan, S. C. (2009) Synthesis and biological evaluation of novel 1-(4-methoxyphenethyl)-1H-benzimidazole-5-carboxylic acid derivatives and their precursors as antileukemic agents. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 19 (16). pp. 4594-4600. ISSN 1464-3405
Full text not available from this repository. (Request a copy)Abstract
We report here the synthesis and preliminary evaluation of novel 1-(4-methoxyphenethyl)-1H-benzimidazole-5-carboxylic acid derivatives 6(a-k) and their precursors 5(a-k) as potential chemotherapeutic agents. In each case, the structures of the compounds were determined by FTIR, H-1 NMR and mass spectroscopy. Among the synthesized molecules, methyl 1-(4-methoxyphenethyl)-2-(4-fluoro-3-nitrophenyl)-1H-benzimidazole-5-car boxylate (5a) induced maximum cell death in leukemic cells with an IC50 value of 3 mu M. Using FACS analysis we show that the compound 5a induces S/G2 cell cycle arrest, which was further supported by the observed down regulation of CDK2, Cyclin B1 and PCNA. The observed downregulation of proapoptotic proteins, upregulation of antiapoptotic proteins, cleavage of PARP and elevated levels of DNA strand breaks indicated the activation of apoptosis by 5a. These results suggest that 5a could be a potent anti-leukemic agent. (C) 2009 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | Benzimidazole-5-carboxylic acid; Anticancer drugs; Chemotherapy; Cancer therapeutics; Apoptosis; DNA damage |
| Subjects: | C Chemical Science > Chemistry |
| Divisions: | Department of > Chemistry |
| Depositing User: | Users 19 not found. |
| Date Deposited: | 19 Aug 2019 10:34 |
| Last Modified: | 25 Oct 2019 09:55 |
| URI: | http://eprints.uni-mysore.ac.in/id/eprint/6770 |
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