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 › peer-review

12 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

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.2174/1871520616666160204113536

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title = "Naphthoflavones as antiproliferative agents: Design, synthesis and biological evaluation",

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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T1 - Naphthoflavones as antiproliferative agents

T2 - Design, synthesis and biological evaluation

AU - Kumar, Dinesh

AU - Singh, Onkar

AU - Nepali, Kunal

AU - Bedi, P. M.S.

AU - Qayum, Arem

AU - Singh, Shashank

AU - Jain, Subheet K.

PY - 2016/7/1

Y1 - 2016/7/1

N2 - 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.

AB - 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.

KW - Apoptosis

KW - Cell lines

KW - Cytotoxicity

KW - Design

KW - Naphthoflavones

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JO - Anti-Cancer Agents in Medicinal Chemistry

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ER -

Naphthoflavones as antiproliferative agents: Design, synthesis and biological evaluation

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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