Synthetic Flavonols and Flavones: a Future Perspective as Anticancer Agents. | [Pakistan Journal of Pharmaceutical Sciences • 2019]

Author(s):

1. Mohammad Shoaib: Department of Pharmacy, University of Malakand, Chakdara, Dir Lower, KPK, Pakistan

2. Mehreen Ghias: Department of Pharmacy, University of Malakand, Chakdara, Dir Lower, KPK, Pakistan

3. Syed Wadood Ali Shah: Department of Pharmacy, University of Malakand, Chakdara, Dir Lower, KPK, Pakistan

4. Niaz Ali: Department of Pharmacology, Institute of Basic Medical Sciences, Khyber Medical University, Peshawar, KPK, Pakistan

5. Muhammad Naveed Umar: Department of Chemistry, University of Malakand, Chakdara, Dir Lower, KPK, Pakistan

6. Meboobur Rahman: Department of Pharmacy, University of Malakand, Chakdara, Dir Lower, KPK, Pakistan

7. Ismail Shah: Department of Pharmacy, University of Malakand, Chakdara, Dir Lower, KPK, Pakistan

8. Shafiullah: Department of Pharmacy, University of Malakand, Chakdara, Dir Lower, KPK, Pakistan

9. Abdullah: Department of Pharmacy, University of Malakand, Chakdara, Dir Lower, KPK, Pakistan

Abstract:

A series of flavonoid derivatives, flavones (F1-F3) and flavonols (OF1-OF3) were synthesized. Their structures were confirmed through various spectroscopic techniques and elemental analysis. These were then tested for cytotoxic activity against mouse fibroblast (NIH 3T3), human endothelial cervical (HeLa) and breast (MCF7) cell lines in vitro by MTT assay. The flavonol series showed prominent potentials than the flavones. The compound OF2 in flavonols exhibited greater potentials MCF7 cell with IC50 value of 0.96µM and OF3 has 1.04µM. In contrast, the OF3 exhibited higher activity against HeLa cell with IC50 value of 0.51µM and OF2 has 1.06µM. The compounds OF2 and OF3 exhibited activity against mouse fibroblast (NIH 3T3) cell with IC50 values 2.48 and 1.24µM. The OF1 was found to be moderate to inactive against all cells. Cytotoxic screening of the tested flavones, F1 to F3 were also active against all cells but the activity was less in comparison to flavonol series of compounds suggestion the possible involvement of hydroxyl (OH) at position 3 in case of flavonols. These results indicated a cheering scaffold that may lead to innovation of potent anti-breast cancer activity.

Page(s): 1081-1089

DOI: DOI not available

Published: Journal: Pakistan Journal of Pharmaceutical Sciences, Volume: 32, Issue: 3, Year: 2019

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