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

doi:10.2174/1871520616666160204113536

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 journal › Article

5 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 language	English
Pages (from-to)	881-890
Number of pages	10
Journal	Anti-Cancer Agents in Medicinal Chemistry
Volume	16
Issue number	7
DOIs	https://doi.org/10.2174/1871520616666160204113536
Publication status	Published - Jul 1 2016
Externally published	Yes

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Keywords

Apoptosis
Cell lines
Cytotoxicity
Design
Naphthoflavones

ASJC Scopus subject areas

Molecular Medicine
Pharmacology
Cancer Research

Cite this

Kumar, D., Singh, O., Nepali, K., Bedi, P. M. S., Qayum, A., Singh, S., & Jain, S. K. (2016). Naphthoflavones as antiproliferative agents: Design, synthesis and biological evaluation. Anti-Cancer Agents in Medicinal Chemistry, 16(7), 881-890. https://doi.org/10.2174/1871520616666160204113536

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AU - Jain, Subheet K.

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10.2174/1871520616666160204113536