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 language | English (US) |
|---|---|
| Pages (from-to) | 3907-3915 |
| Number of pages | 9 |
| Journal | Medicinal Chemistry Research |
| Volume | 23 |
| Issue number | 8 |
| DOIs | |
| State | Published - Jan 1 2014 |
| Externally published | Yes |
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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 journal › Article
}
TY - JOUR
T1 - In-vitro cytotoxicity, antioxidant, bleomycin-dependent DNA damage and immunomodulatory evaluation of 1-(4-acetylphenyl)-3-aryloxypyrrolidine-2,5-dione based derivatives
AU - Patel, Jigarkumar R.
AU - Dhorajiya, Bhaveshkumar D.
AU - Dholakiya, Bharatkumar Z.
AU - Badria, Farid A.
AU - Ibrahim, Ahmed Salah
PY - 2014/1/1
Y1 - 2014/1/1
N2 - 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.
AB - 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.
KW - Antioxidant
KW - Bleomycin-dependent DNA damage
KW - Cytotoxicity
KW - Lymphocyte transformation
KW - Oxa-michael adducts
UR - http://www.scopus.com/inward/record.url?scp=84904445304&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84904445304&partnerID=8YFLogxK
U2 - 10.1007/s00044-014-0965-5
DO - 10.1007/s00044-014-0965-5
M3 - Article
AN - SCOPUS:84904445304
VL - 23
SP - 3907
EP - 3915
JO - Medicinal Chemistry Research
JF - Medicinal Chemistry Research
SN - 1054-2523
IS - 8
ER -