Sridhara, M. B. and Rakesh, K. P. and Manukumar, H. M. and Shantharam, C. S. and Hamse K. Vivek and Kumara, H. K. and Yasser H.E. Mohammed and Gowda, Dale C. (2020) Synthesis of Dihydrazones as Potential Anticancer and DNA Binding Candidates: A Validation by Molecular Docking Studies. Anti-Cancer Agents in Medicinal Chemistry, 20 (7). pp. 845-858. ISSN 1875-5992
Full text not available from this repository. (Request a copy)Abstract
Background: Accounting for mortality nearly one in four of human and second highest leading cause of death worldwide. Every year, about 10 million new cancers are diagnosed and causing major health issues in both developing and developed countries. Methods: A series of new dihydrazones were synthesized and screened for in vitro anticancer activity against three different MDA-MB-231, A546 and MCF7 cell lines and validated by DNA binding and molecular docking approaches. Result: In the present investigations, synthesized compounds 21, 22, 23 and 24 exhibited potent anticancer activity against tested cancer cell lines and DNA binding study using methyl green comparing to Doxorubicin and ethidium bromide as a positive control respectively. Conclusion: The Structure Activity Relationship (SAR) showed that the electron withdrawing groups (-Cl, -NO2, -F, and -Br) favored the DNA binding studies and anticancer activity whereas, electron donating groups (-OH and -OCH3) showed moderate activity. In the molecular docking study, binding interactions of the most active compounds 21, 22, 23 and 24 stacked with A-T rich regions of the DNA minor groove by surface binding interactions were confirmed. Further, the tuning of active analogs for targeted therapy was warranted.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | Dihydrazones; anticancer; DNA binding studies; docking study; MDA-MB-231; A546; MCF7 |
| Subjects: | C Chemical Science > Chemistry |
| Divisions: | Department of > Chemistry |
| Depositing User: | Mr Umendra uom |
| Date Deposited: | 03 Feb 2021 06:11 |
| Last Modified: | 16 Jul 2022 06:25 |
| URI: | http://eprints.uni-mysore.ac.in/id/eprint/15659 |
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