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 | |
| 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
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 journal › Article
}
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 -