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Synthesis, molecular docking, cytotoxicity and antioxidant activity evaluation of 4-(3-chloro-1, 4- dioxo-1, 4-dihydronaphthalen-2-ylamino) benzenesulfonamide derivatives
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| Author:
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PALANICHAMY SANTHOSH 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, 3-
dichloronaphthalene -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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| DOI:
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