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

6 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

Keywords

Apoptosis
Cell lines
Cytotoxicity
Design
Naphthoflavones

ASJC Scopus subject areas

Molecular Medicine
Pharmacology
Cancer Research

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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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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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AU - Kumar, Dinesh

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AU - Nepali, Kunal

AU - Bedi, P. M.S.

AU - Qayum, Arem

AU - Singh, Shashank

AU - Jain, Subheet K.

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