Naphthoflavones as Antiproliferative Agents: Design, Synthesis and Biological Evaluation

Author(s):

Dinesh Kumar, Onkar Singh, Kunal Nepali, PMS Bedi, Arem Qayum, Shashank Singh and Subheet K. Jain   Pages 881 - 890 ( 10 )

Abstract:

The present study involves the design and synthesis of naphthoflavones as antiproliferative agents. The strategy presents naphthoflavones as hybrids of naphthyl based chalcones and flavones. A panel of human cancer cell lines were employed for the cytotoxicity studies. DK-13 exhibited significant cytoxicity against MiaPaCa-2 cell lines with IC50 value of 1.93 μM and 5.63 μM against MCF-7 cell lines. The compound DK-13 was found to induce apoptosis evidenced through phase contrast microscopy, DAPI staining, and mitochondrial membrane potential loss. The cell phase distribution studies indicated an increase from 11.26 % (control sample) to 55.19 % (sample treated with 20 μM compound DK-13) in the apoptotic population.

Keywords:

Apoptosis, naphthoflavones, cytotoxicity, cell lines, design.

Affiliation:

, , , , , , Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, Punjab-143005.

Graphical Abstract:

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