New ferrocenyl guanidines as potent antioxidants, protein kinase inhibitors and cytotoxic agents against human leukemia THP-1 cell line
- Авторы: Gul R.1, Badshah A.1, Altaf A.1, Tabassum S.2, Zia M.2
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Учреждения:
- Department of Chemistry
- Department of Biotechnology
- Выпуск: Том 87, № 11 (2017)
- Страницы: 2684-2689
- Раздел: Article
- URL: https://journals.rcsi.science/1070-3632/article/view/221621
- DOI: https://doi.org/10.1134/S1070363217110251
- ID: 221621
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Аннотация
Six new ferrocenyl guanidines were synthesized and characterized by elemental analysis, FT-IR and 1H and 13C NMR. Compounds 1–6 were screened for antioxidant, protein kinase inhibition, lethality of brine shrimp, and cytotoxicity against the human leukemia THP-1 cell line. The compounds demonstrated moderate to significant activities. Antioxidant activity of the synthesized compounds was evaluated by DPPH % inhibition with IC50 values. All compounds 1–6 showed notable antioxidant activity with DPPH having IC50 values between 23.2–15.1 and noteworthy brine shrimp lethality. Compound 6 demonstrated the highest cytotoxicity against brine shrimps with LC50 of 9.09 μg/mL. Protein kinase inhibition activity showed significant hyphea formation inhibition at 100 μg/disc with 10 to 13 mm clear zone of inhibition for the compounds 2–6. The compounds were screened for in vitro cytotoxicity using human leukemia cell line (THP-1 ATCC#TIB-202). Among all compounds, the most significant activity was demonstrated by compounds 6 and 5 with IC50 of 3.88 and 5.59 μg/mL which was comparable with the standard 5-flourouracil and vincristine drugs.
Об авторах
R. Gul
Department of Chemistry
Автор, ответственный за переписку.
Email: rukh_sanna@yahoo.com
Пакистан, Kohat, 26000
A. Badshah
Department of Chemistry
Email: rukh_sanna@yahoo.com
Пакистан, Islamabad, 45320
A. Altaf
Department of Chemistry
Email: rukh_sanna@yahoo.com
Пакистан, Gujrat, 50700
S. Tabassum
Department of Biotechnology
Email: rukh_sanna@yahoo.com
Пакистан, Islamabad, 45320
M. Zia
Department of Biotechnology
Email: rukh_sanna@yahoo.com
Пакистан, Islamabad, 45320