Naphthoflavones as antiproliferative agents

Design, synthesis and biological evaluation

Dinesh Kumar, Onkar Singh, Kunal Nepali, P. M.S. Bedi, Arem Qayum, Shashank Singh, Subheet K. Jain

Research output: Contribution to journalArticle

4 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)881-890
Number of pages10
JournalAnti-Cancer Agents in Medicinal Chemistry
Volume16
Issue number7
DOIs
Publication statusPublished - Jul 1 2016
Externally publishedYes

Fingerprint

Cell Line
Chalcones
Flavones
Phase-Contrast Microscopy
Mitochondrial Membrane Potential
MCF-7 Cells
Inhibitory Concentration 50
Apoptosis
Staining and Labeling
Population
Neoplasms
DAPI
compound 20

Keywords

  • Apoptosis
  • Cell lines
  • Cytotoxicity
  • Design
  • Naphthoflavones

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Cancer Research

Cite this

Naphthoflavones as antiproliferative agents : Design, synthesis and biological evaluation. / Kumar, Dinesh; Singh, Onkar; Nepali, Kunal; Bedi, P. M.S.; Qayum, Arem; Singh, Shashank; Jain, Subheet K.

In: Anti-Cancer Agents in Medicinal Chemistry, Vol. 16, No. 7, 01.07.2016, p. 881-890.

Research output: Contribution to journalArticle

Kumar, Dinesh ; Singh, Onkar ; Nepali, Kunal ; Bedi, P. M.S. ; Qayum, Arem ; Singh, Shashank ; Jain, Subheet K. / Naphthoflavones as antiproliferative agents : Design, synthesis and biological evaluation. In: Anti-Cancer Agents in Medicinal Chemistry. 2016 ; Vol. 16, No. 7. pp. 881-890.
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