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Synthesis, molecular docking, cytotoxicity and antioxidant activity evaluation of 4- (3- chloro-1, 4-dioxo-1, 4-dihydronaphthalen-2ylamino ) benzenesulfonamide derivatives
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| Author:
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PALANICHAMY KUMAR, KURUBA BHARATH KUMAR, ASIR OBADIAH, RAMAN MOHANAPRIYA , ARULAPPAN DURAIRAJ , SUBRAMANIAN RAMANATHAN , SAMUEL VASANTHKUMAR
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| Abstract:
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A variety of acyl chlorides and 4-aminobenzenesulfonamide have been employed to functionalize 2, 3dichloronaphthalene
-1, 4-dione
to obtain 4-
(3-chloro-1, 4-dioxo-1, 4-dihydronaphthalen-2-ylamino
)
benzenesulfonamide derivatives. All the synthesized compounds are screened for their bioactivity through molecular
docking, cytotoxicity
(against HeLa
) and antioxidant activity. DPPH and ABTS evaluation procedures are employed to
assess the antioxidant activity. Among the synthesized 4-
(3-chloro-1, 4-dioxo-1, 4-dihydronaphthalen-2-ylamino
)
benzenesulfonamide derivatives
(3, 4, 5a-f
), the compound 4 exhibited the highest inhibition of 75% and 82% in the
DPPH and ABTS antioxidant activity evaluation respectively. The compounds 5b and 5c has exhibited better binding
energy when docked with HDAC8. Cytotoxicity of the synthesized compounds was studied against cervical cancer
cell line
(HeLa
) and compounds 4 and 5e showed the maximum inhibition and displayed a better activity than the
standard drug.
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| Keyword:
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4- (3-chloro-1, 4-dioxo-1, 4-dihydronaphthalen-2-ylamino ) benzenesulfonamide; Molecular docking; cytotoxicity; HeLa cell lines; antioxidant activity.
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| EOI:
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| DOI:
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https://doi.org/10.31838/ijpr/2020.12.01.014
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| Download:
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