Title:Naphthoflavones as Antiproliferative Agents: Design, Synthesis and Biological Evaluation
Volume: 16
Issue: 7
Author(s): Dinesh Kumar, Onkar Singh, Kunal Nepali, PMS Bedi, Arem Qayum, Shashank Singh and Subheet K. Jain
Affiliation:
Keywords:
Apoptosis, naphthoflavones, cytotoxicity, cell lines, design.
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.