Cytotoxic Activity of Flavone Analogues

Authors

  • Dr. Afroze Alam
  • U Farooq Faculty of Dentistry, Taif University, Taif, Kingdom of Saudi Arabia.
  • Kamlesh Kumar Naik Nandha College of Pharmacy, Perundurai Main Road, Erode, Tamil Nadu-638052, India.
  • Rashmi Singh Narayan Institute of Pharmacy, Jamuhar, Sasaram (ROHTAS) 821305, Bihar, India.
  • Vachaspati Dubey Narayan Institute of Pharmacy, Jamuhar, Sasaram (ROHTAS) 821305, Bihar, India.
  • Monika Verma Department of Paediatrics, Advance Paediatrics Centre, PGIMER, Chandigarh, Punjab-160012.
  • B D Tripathi Narayan Institute of Pharmacy, Jamuhar, Sasaram (ROHTAS) 821305, Bihar, India.
  • Vinod Kumar Narayan Institute of Pharmacy, Jamuhar, Sasaram (ROHTAS) 821305, Bihar, India.

Keywords:

Benzopyrone, Cytotoxic activity, Flavonoids, HeLa cell line, log ‘P’ value, MTT assay

Abstract

The flavonoids are polyphenolic compounds and universally present as constituents of flowering plants,
particularly of food plants. The flavonoids are phenyl substituted chroman (benzopyran derivatives) consisting
of a 15-carbon basic skeleton (C6-C3-C6), composed of a chroman (C6-C3) nucleus (the benzo ring A and
the heterocyclic ring C), also shared by the tocopherols, with a phenyl (the aromatic ring B), substitution
usually at the 2-position. Different substitutions can typically occur in the rings, A and B. Several plants
and spices containing flavonoid derivatives have found application as disease preventive and therapeutic
agents in traditional medicine in Asia for thousands of years. Various analogues of 3-methylflavones
were synthesised, purified and characterised by UV, IR, 1HNMR and mass spectrometry .All the synthesised
compounds were evaluated for their cytotoxic activity by MTT assay against HeLa cell line. Most of the
compounds show moderate activity, whereas the compounds like FA-04.FA-20,FA-10 and FA-13 have
shown good activity having IC50 value 22.00,25.49.26.24 and 26.35 ?g/ml respectively, in comparison
to standard molecule Cisplastin had IC50 value 6- 12.5 ?g/ml . Thus it appears the presence of 3- methyl
group in the flavone nucleus significantly influences the log ‘P’ value of all the twenty test compounds.

The prominent activity the of above compounds is probably because of 3-methyl and N, N-dimethyl amino
substitution on 4’- position of flavonoid nucleus.

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Published

2018-10-26

How to Cite

Alam, D. A., Farooq, U., Naik, K. K., Singh, R., Dubey, V., Verma, M., Tripathi, B. D., & Kumar, V. (2018). Cytotoxic Activity of Flavone Analogues. Journal of Drug Discovery and Development ( ISSN:2581-6861), 1(1), 13-21. Retrieved from http://www.medicaljournalshouse.com/index.php/JDrug-Discovery-Development/article/view/49

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Vol. 1 No. 1 (2017): Journal of Drug Discovery and Development

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