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INTERNATIONAL JOURNAL OF PHARMACEUTICAL RESEARCH

A Step Towards Excellence
Published by : Advanced Scientific Research
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0975-2366
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IJPR 9[3] July - September 2017 Special Issue

July - September 9[3] 2017

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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

Author: PALANICHAMY SANTHOSH KUMAR, KURUBA BHARATH KUMAR, ASIR OBADIAH, RAMAN MOHANAPRIYA, ARULAPPAN DURAIRAJ, SUBRAMANIAN RAMANATHAN, SAMUEL VASANTHKUMAR
Abstract: 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.
Keyword: 4-(3-chloro-1, 4-dioxo-1, 4-dihydronaphthalen-2-ylamino) benzenesulfonamide; Molecular docking; cytotoxicity; HeLa cell lines; antioxidant activity.
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