Naphthoflavones as Antiproliferative Agents: Design, Synthesis and Biological Evaluation

Author(s): Dinesh Kumar, Onkar Singh, Kunal Nepali, PMS Bedi, Arem Qayum, Shashank Singh, Subheet K. Jain

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 16 , Issue 7 , 2016

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Graphical 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.

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Article Details

Year: 2016
Published on: 19 May, 2016
Page: [881 - 890]
Pages: 10
DOI: 10.2174/1871520616666160204113536
Price: $65

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