TY - JOUR
T1 - Synthesis, molecular docking, cytotoxicity and antioxidant activity evaluation of 4-(3-chloro-1, 4-dioxo-1, 4-dihydronaphthalen-2-ylamino) benzenesulfonamide derivatives
AU - Kumar, Palanichamy Santhosh
AU - Kumar, Kuruba Bharath
AU - Obadiah, Asir
AU - Mohanapriya, Raman
AU - Durairaj, Arulappan
AU - Ramanathan, Subramanian
AU - Vasanthkumar, Samuel
N1 - Publisher Copyright:
© 2020, Advanced Scientific Research. All rights reserved.
PY - 2020/1/1
Y1 - 2020/1/1
N2 - 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.
AB - 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.
KW - 4-(3-chloro-1, 4-dioxo-1, 4-dihydronaphthalen-2-ylamino) benzenesulfonamide
KW - Antioxidant activity
KW - Cytotoxicity
KW - HeLa cell lines
KW - Molecular docking
UR - http://www.scopus.com/inward/record.url?scp=85090615801&partnerID=8YFLogxK
U2 - 10.31838/ijpr/2020.12.01.014
DO - 10.31838/ijpr/2020.12.01.014
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AN - SCOPUS:85090615801
SN - 0975-2366
VL - 12
SP - 134
EP - 168
JO - International Journal of Pharmaceutical Research
JF - International Journal of Pharmaceutical Research
IS - 1
ER -
