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Anti-Cancer Agents in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

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

Volume 16, Issue 7, 2016

Page: [881 - 890] Pages: 10

DOI: 10.2174/1871520616666160204113536

Price: $65

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.

Graphical Abstract

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