SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY OF ACRIDINE-SULFONAMIDE CONJUGATES
Journal Title: European Journal of Pharmaceutical and Medical Research - Year 2018, Vol 5, Issue 5
Abstract
The present study describes the synthesis and antiproliferative evaluation of several acridine analogues carrying sulfonamide and thiouredoside chain at C-9 position. The key intermediate aminoacridines5 were prepared by nucleophilic aromatic substitution (SNAr) of 9-chloroacridine 4 with 4,4'-diaminodiphenylmethane or p-phenylenediamine. The 9-amino derivatives 5 were further reacted with phenylisothiocyanate or arylsulfonlychloridesto afford the corresponding thiourea-, or acridine sulfonamide analogues6 and 7 respectively. Some of the prepared derivatives showed a strong antiproliferative activity against the breast, colon and hepatocellular carcinoma cell lines. Among them, compounds 5b and 8bwere the most potentwith IC50 values 5.88, 8.30, 8.93 and 8.83, 14.51, 9.39 against breast, hepatocellular and coloncarcinoma cell lines respectively.
Authors and Affiliations
Prof. Dr. Ibrahim El Tantawy El Sayed
Keywords
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