Saravana Priya, D (2018) Design, Synthesis, Characterization, Molecular Docking Studies and Biological Evaluation of Benzimidazole Containing 4H-Chromen-4-one Derivatives. Masters thesis, J.K.K.Nattraja College of Pharmacy, Komarapalayam.
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Abstract
The present study deals with designing of some novel (E)-2-(2-(5-nitro-1Hbenzo[d]imidazol-2-yl)vinyl)-4H-chromen-4-one Derivatives on the basis reaction between 2-methyl-1H-benzo[d]imidazole, substituted chromone-3-carbaldehyde in presence of GAA. • The synthesized compound were characterized by IR, 1H NMR, 13C NMR, Mass spectrometry and Elementary Analysis. • Preliminary QSAR study was carried out for the synthesized compounds. All the compounds obey the Lipnski rule of 5. • Solubility characters of synthesized compounds were carried out by using various solvents. The tested compounds are freely soluble in DMSO, soluble in Chloroform and Methanol, slightly soluble in Acetone, Ethyl Acetate and Ethanol and Insoluble in Water. • The structures of the synthesized compounds were studied using Autodock software against different target enzymes. The docking results showed that Compounds R2, R3, R6, and R7 were found to have significant binding score against target enzyme MAP Kinase compared to standard drug Imatinib. • Synthesized compound were evaluated for their in-vitro anti cancer activity by SRB assay method against Human Cancer Cell line A-549. From the result the compound R1 and R6 allowed only 21.9 and 39.4 of % cell growth at the concentration of 80μg/mL. Whereas other compounds has showed 57-94% 0f %cell growth. • From the above, it may conclude that the substitution on the Coumarin nucleus alter the biological activity. The un-substituted (R4) and Flouro (R6) and Chloro (R1) substituted Coumarin derivatives were found to be potent by producing biological activity.
| Item Type: | Thesis (Masters) |
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| Additional Information: | Reg.No: 261615206 |
| Uncontrolled Keywords: | Benzimidazole ; 4H-Chromen-4-one Derivatives ; Design ; Synthesis ; Characterization ; Molecular Docking Studies ; Biological Evaluation. |
| Subjects: | PHARMACY > Pharmaceutical Chemistry |
| Depositing User: | Subramani R |
| Date Deposited: | 28 Jun 2019 02:01 |
| Last Modified: | 28 Jun 2019 02:01 |
| URI: | http://repository-tnmgrmu.ac.in/id/eprint/10630 |
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