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
Anti-Cancer Agents in Medicinal Chemistry
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.
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Cite this article as:
Kumar Dinesh, Singh Onkar, Nepali Kunal, Bedi PMS, Qayum Arem, Singh Shashank and K. Jain Subheet, Naphthoflavones as Antiproliferative Agents: Design, Synthesis and Biological Evaluation, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (7) . https://dx.doi.org/10.2174/1871520616666160204113536
DOI https://dx.doi.org/10.2174/1871520616666160204113536 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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