Research Article | Volume: 6, Issue: 12, December, 2016

Synthesis, bioactivity and Docking Study of Some New Indole-hydrazone Derivatives

N. Sharaf El-Dina A. Barseemb   

Open Access   

Published:  Dec 28, 2016

DOI: 10.7324/JAPS.2016.601211

In the present study, a series of new indole-hydrazone derivatives were synthesized. The structures of the synthesized compounds were established on the basis of elemental and spectral (IR and 1H-NMR) studies. All synthesized compounds were screened for their anti-inflammatory against carrageenan induced oedema in albino rats at a dose of 0.2 mmol/kg using indomethacin as a standard drug. The reduction in oedema formation was ranged between 72.3 – 89.3 % for all the synthesized compounds compared to indomethacin (46 % inhibition). Moreover, their anticancer activity against breast cancer cell line (MCF-7) at a dose of 100µg/ml was evaluated. The compounds 2f and 2j showed mild anticancer activity (61% and 68% inhibition, respectively) compared to doxorubicin. Furthermore, all molecules were docked to the active site of both cox-1 and cox-2 using the docking program Molego virtual docker. All prepared compounds showed high docking score against both cox-1 and cox-2. The dock scores and binding energy were found to be in good agreement with the pharmacological results. Finally, the drug likeness and bioactivity were predicted using Molinspiration software. The results revealed that all new compounds show good drug likeness score and bioactivity score.

Keyword:     Indole Hydrazone Anticancer Anti-inflammatory molecular docking drug likeness and bioactivity.


Sharaf El-Din N., Barseem A. Synthesis, bioactivity and Docking Study of Some New Indole-h

Copyright:The Author(s). This is an open access article distributed under the Creative Commons Attribution Non-Commercial License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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