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

7 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

Access to Document

10.2174/1871520616666160204113536

Fingerprint Dive into the research topics of 'Naphthoflavones as antiproliferative agents: Design, synthesis and biological evaluation'. Together they form a unique fingerprint.

Cite this

@article{066d6e220e684b70ac7ebc73e4afd727,

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.",

keywords = "Apoptosis, Cell lines, Cytotoxicity, Design, Naphthoflavones",

author = "Dinesh Kumar and Onkar Singh and Kunal Nepali and Bedi, {P. M.S.} and Arem Qayum and Shashank Singh and Jain, {Subheet K.}",

year = "2016",

month = jul,

day = "1",

doi = "10.2174/1871520616666160204113536",

language = "English",

volume = "16",

pages = "881--890",

journal = "Anti-Cancer Agents in Medicinal Chemistry",

issn = "1871-5206",

publisher = "Bentham Science Publishers B.V.",

number = "7",

}

TY - JOUR

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

UR - http://www.scopus.com/inward/record.url?scp=84973622616&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84973622616&partnerID=8YFLogxK

U2 - 10.2174/1871520616666160204113536

DO - 10.2174/1871520616666160204113536

M3 - Article

C2 - 26845133

AN - SCOPUS:84973622616

VL - 16

SP - 881

EP - 890

JO - Anti-Cancer Agents in Medicinal Chemistry

JF - Anti-Cancer Agents in Medicinal Chemistry

SN - 1871-5206

IS - 7

ER -