In Vitro cytotoxicity and antioxidant evaluation of 7-amino-2-styrylchromone derivatives

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Abstract

Objective: The objective of this study was to synthesize 7-amino-2-styrylchromone derivatives and evaluate their in vitro cytotoxic and antioxidant potential. Methods: 7-amino-2-styrylchromones were synthesized from 7-amino-2-methylchromone by condensing it with various substituted aromatic aldehydes. The cytotoxicity of the synthesized molecules was assessed against two cell lines, MCF-7 and HCT-116 by 3-(4,5-dimethyl thiazol-2-yl)-2,5- diphenyl tetrazolium bromide assay. Cell cycle analysis of the most potent molecule ASC-7 was carried out. The antioxidant studies were conducted by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide methods. Result: (E)-7-amino-2-(3,4-methylenedioxystyryl)-4H-chromen-4-one (ASC-7) with inhibitory concentration 50% (IC50) 56.0 µM was found to be the most potent molecule against MCF-7. ASC-7 induced G0/G1 phase arrest of MCF-7. Furthermore, (E)-7-amino-2-(3,4-methylenedioxystyryl)- 4H-chromen-4-one(ASC-7) showed good DPPH scavenging activity (IC50 54.6 µM). However, none of the tested compounds exhibited nitric oxide scavenging property. Conclusion: This study reports the synthesis of 7-amino-2-styrylchromones. Some of the synthesized compounds showed moderate cytotoxicity against the tested cell lines MCF-7 and HCT-116. (E)-7-amino-2-(3,4-methylenedioxystyryl)-4H-chromen-4-one (ASC-7) was found to be the best cytotoxic and antioxidant agent.

Original languageEnglish
Pages (from-to)152-156
Number of pages5
JournalAsian Journal of Pharmaceutical and Clinical Research
Volume10
Issue number11
DOIs
Publication statusPublished - 01-11-2017

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Antioxidants
Inhibitory Concentration 50
Nitric Oxide
Cell Line
Cell Cycle Resting Phase
Cytotoxins
G1 Phase
Bromides
Aldehydes
Cell Cycle
2-styrylchromone
In Vitro Techniques
2,2-diphenyl-1-picrylhydrazyl
diphenyl

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmaceutical Science
  • Pharmacology (medical)

Cite this

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title = "In Vitro cytotoxicity and antioxidant evaluation of 7-amino-2-styrylchromone derivatives",
abstract = "Objective: The objective of this study was to synthesize 7-amino-2-styrylchromone derivatives and evaluate their in vitro cytotoxic and antioxidant potential. Methods: 7-amino-2-styrylchromones were synthesized from 7-amino-2-methylchromone by condensing it with various substituted aromatic aldehydes. The cytotoxicity of the synthesized molecules was assessed against two cell lines, MCF-7 and HCT-116 by 3-(4,5-dimethyl thiazol-2-yl)-2,5- diphenyl tetrazolium bromide assay. Cell cycle analysis of the most potent molecule ASC-7 was carried out. The antioxidant studies were conducted by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide methods. Result: (E)-7-amino-2-(3,4-methylenedioxystyryl)-4H-chromen-4-one (ASC-7) with inhibitory concentration 50{\%} (IC50) 56.0 µM was found to be the most potent molecule against MCF-7. ASC-7 induced G0/G1 phase arrest of MCF-7. Furthermore, (E)-7-amino-2-(3,4-methylenedioxystyryl)- 4H-chromen-4-one(ASC-7) showed good DPPH scavenging activity (IC50 54.6 µM). However, none of the tested compounds exhibited nitric oxide scavenging property. Conclusion: This study reports the synthesis of 7-amino-2-styrylchromones. Some of the synthesized compounds showed moderate cytotoxicity against the tested cell lines MCF-7 and HCT-116. (E)-7-amino-2-(3,4-methylenedioxystyryl)-4H-chromen-4-one (ASC-7) was found to be the best cytotoxic and antioxidant agent.",
author = "Lalitha Simon",
year = "2017",
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doi = "10.22159/ajpcr.2017.v10i11.20587",
language = "English",
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T1 - In Vitro cytotoxicity and antioxidant evaluation of 7-amino-2-styrylchromone derivatives

AU - Simon, Lalitha

PY - 2017/11/1

Y1 - 2017/11/1

N2 - Objective: The objective of this study was to synthesize 7-amino-2-styrylchromone derivatives and evaluate their in vitro cytotoxic and antioxidant potential. Methods: 7-amino-2-styrylchromones were synthesized from 7-amino-2-methylchromone by condensing it with various substituted aromatic aldehydes. The cytotoxicity of the synthesized molecules was assessed against two cell lines, MCF-7 and HCT-116 by 3-(4,5-dimethyl thiazol-2-yl)-2,5- diphenyl tetrazolium bromide assay. Cell cycle analysis of the most potent molecule ASC-7 was carried out. The antioxidant studies were conducted by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide methods. Result: (E)-7-amino-2-(3,4-methylenedioxystyryl)-4H-chromen-4-one (ASC-7) with inhibitory concentration 50% (IC50) 56.0 µM was found to be the most potent molecule against MCF-7. ASC-7 induced G0/G1 phase arrest of MCF-7. Furthermore, (E)-7-amino-2-(3,4-methylenedioxystyryl)- 4H-chromen-4-one(ASC-7) showed good DPPH scavenging activity (IC50 54.6 µM). However, none of the tested compounds exhibited nitric oxide scavenging property. Conclusion: This study reports the synthesis of 7-amino-2-styrylchromones. Some of the synthesized compounds showed moderate cytotoxicity against the tested cell lines MCF-7 and HCT-116. (E)-7-amino-2-(3,4-methylenedioxystyryl)-4H-chromen-4-one (ASC-7) was found to be the best cytotoxic and antioxidant agent.

AB - Objective: The objective of this study was to synthesize 7-amino-2-styrylchromone derivatives and evaluate their in vitro cytotoxic and antioxidant potential. Methods: 7-amino-2-styrylchromones were synthesized from 7-amino-2-methylchromone by condensing it with various substituted aromatic aldehydes. The cytotoxicity of the synthesized molecules was assessed against two cell lines, MCF-7 and HCT-116 by 3-(4,5-dimethyl thiazol-2-yl)-2,5- diphenyl tetrazolium bromide assay. Cell cycle analysis of the most potent molecule ASC-7 was carried out. The antioxidant studies were conducted by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide methods. Result: (E)-7-amino-2-(3,4-methylenedioxystyryl)-4H-chromen-4-one (ASC-7) with inhibitory concentration 50% (IC50) 56.0 µM was found to be the most potent molecule against MCF-7. ASC-7 induced G0/G1 phase arrest of MCF-7. Furthermore, (E)-7-amino-2-(3,4-methylenedioxystyryl)- 4H-chromen-4-one(ASC-7) showed good DPPH scavenging activity (IC50 54.6 µM). However, none of the tested compounds exhibited nitric oxide scavenging property. Conclusion: This study reports the synthesis of 7-amino-2-styrylchromones. Some of the synthesized compounds showed moderate cytotoxicity against the tested cell lines MCF-7 and HCT-116. (E)-7-amino-2-(3,4-methylenedioxystyryl)-4H-chromen-4-one (ASC-7) was found to be the best cytotoxic and antioxidant agent.

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SN - 0974-2441

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