Kuthyala, Sharanya and Sheikh, Sareen and Prabhu, Ashwini and Rekha, P. D. and Karikannar, Nagaraja G. and Shankar, Madan K. (2020) Synthesis, Characterization, and Anticancer Studies of Some Pyrazole-Based Hybrid Heteroatomics. Chemistryselect, 5 (35). pp. 10827-10834. ISSN 2365-6549
Full text not available from this repository. (Request a copy)Abstract
Defined with a dual-mode of action, the hybrid molecule synthesis is an attractive strategy to endure the scientific challenges in drug discovery. Besides worthy development in cancer therapy, it is still a leading cause of death across the globe. Failure in terms of efficacy, selectivity and toxicity, the statistics of a potential drug to concrete the cancer is rather in bleak. In the present study, synthesized hybrid molecules were well characterized by spectroscopy techniques. The single-crystal X-ray crystallography study revealed the monoclinic crystal system of Dimethyl 1,4-dihydro-2,6-dimethyl-4-(3-(5-methyl-1-phenyl-1H-pyrazol-4-yl)-1H-pyr azol-4-yl)pyridine-3,5-dicarboxylate (5 b) with spacegroupC2/c. MTT assay provided the anticancer property of the compounds Diethyl1,4-dihydro-3,5-dimethyl-4-(3-(5-methyl-1-phenyl-1H-pyrazol-4-yl) -1H-pyrazol-4-yl)pyridine-2,6-dicarboxylate (5 a) and 5-methyl-1-phenyl-4-(4-(4,5-diphenyl-1H-imidazol-2-yl)-1H-pyrazol-3-yl)- 1H-pyrazole (6 a) against A549 cell lines with the IC(50)values of 42.79 mu M and 55.13 mu M respectively. The AO-EB staining assay for cell death analysis confirmed the selective action of both5 aand6 a. Further, molecular docking confirmed the effective binding with cyclin-dependent kinase (CDK2) protein, suggesting that the target compounds are remarkable inhibitors in dysregulating the CDK2 protein in cancer cells.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | Cell death analysis; crystal growth; Docking; Drug discovery; MTT Assay |
| Subjects: | C Chemical Science > Chemistry |
| Divisions: | Department of > Institution of Excellence |
| Depositing User: | Mr Umendra uom |
| Date Deposited: | 01 Apr 2021 10:11 |
| Last Modified: | 01 Apr 2021 10:11 |
| URI: | http://eprints.uni-mysore.ac.in/id/eprint/15511 |
Actions (login required)
 |
View Item |
