In-vitro cytotoxicity, antioxidant, bleomycin-dependent DNA damage and immunomodulatory evaluation of 1-(4-acetylphenyl)-3-aryloxypyrrolidine-2,5-dione based derivatives

Jigarkumar R. Patel, Bhaveshkumar D. Dhorajiya, Bharatkumar Z. Dholakiya, Farid A. Badria, Ahmed Salah Ibrahim

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

A one pot, economical, and efficient synthesis of 1-(4-acetylphenyl)-3- aryloxypyrrolidine-2,5-diones-based derivatives 5a-l have been accomplished in single steps and in satisfactory yields from 1-(4-acetylphenyl)-pyrrole-2,5- diones 3 and phenols 4a-l. All the compounds were characterized by physical, spectroscopic, and elemental analysis. The selection of the bioassays was based on proving the drug receptor binding concept. Compounds 5g, 5k, 5h, 5i, 5a, and 5f showed the highest inhibitory antioxidant activity using ABTS methods. Compounds 5k, 5g, 5c, 5h, 5b, 5d, 5f, and 5j manifested the best protective effect against DNA damage induced by bleomycin. Moreover, an in-vitro cytotoxic activity evaluation of all synthesized compounds was against four cancer cell lines using 5-Fluorouracil as a standard anticancer drug.

Original languageEnglish (US)
Pages (from-to)3907-3915
Number of pages9
JournalMedicinal Chemistry Research
Volume23
Issue number8
DOIs
StatePublished - Jan 1 2014
Externally publishedYes

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Drug Receptors
Pyrroles
Spectroscopic analysis
Bioassay
Phenols
Bleomycin
Cytotoxicity
Fluorouracil
Biological Assay
DNA Damage
Antioxidants
Cells
Derivatives
Cell Line
DNA
Chemical analysis
Pharmaceutical Preparations
Neoplasms
2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid
In Vitro Techniques

Keywords

  • Antioxidant
  • Bleomycin-dependent DNA damage
  • Cytotoxicity
  • Lymphocyte transformation
  • Oxa-michael adducts

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry

Cite this

In-vitro cytotoxicity, antioxidant, bleomycin-dependent DNA damage and immunomodulatory evaluation of 1-(4-acetylphenyl)-3-aryloxypyrrolidine-2,5-dione based derivatives. / Patel, Jigarkumar R.; Dhorajiya, Bhaveshkumar D.; Dholakiya, Bharatkumar Z.; Badria, Farid A.; Ibrahim, Ahmed Salah.

In: Medicinal Chemistry Research, Vol. 23, No. 8, 01.01.2014, p. 3907-3915.

Research output: Contribution to journalArticle

Patel, Jigarkumar R. ; Dhorajiya, Bhaveshkumar D. ; Dholakiya, Bharatkumar Z. ; Badria, Farid A. ; Ibrahim, Ahmed Salah. / In-vitro cytotoxicity, antioxidant, bleomycin-dependent DNA damage and immunomodulatory evaluation of 1-(4-acetylphenyl)-3-aryloxypyrrolidine-2,5-dione based derivatives. In: Medicinal Chemistry Research. 2014 ; Vol. 23, No. 8. pp. 3907-3915.
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