Novel anthracene-9-sulfonyl derivatives as anticancer agents: synthesis and in vitro biological evaluation

Document Type : Original Article

Authors

1 Pharmaceutical Industries Research division Therapeutical Chemistry Department National Research Centre

2 2Department of Therapeutic Chemistry, Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, Cairo, Egypt, 12622.

3 Department of Therapeutic Chemistry, National Research Centre, Dokki 12622, Giza, Egypt,

4 Pharmaceutical and Drug Industries Research Division, Department of Pharmacognosy, National Research Centre, Giza, Egypt

5 Department Of Microbial and Natural Products chemistry National Research Centre

Abstract

In this study, a new series of anthracene-9-sulfonyl derivatives incorporated with different heterocyclic moieties were synthesized and screened for their in vitro anticancer activity against colon carcinoma cell lines (HCT-116), hepatic carcinoma cell lines (HepG 2) and breast carcinoma cell lines (MCF-7). Among them, compound 4-acetylphenyl anthracene-9-sulfonate (8) showed selective high cytotoxic activity over colon carcinoma cell lines (HCT-116), also compounds 2-(anthracen-9-ylsulfonyl)malononitrile (7), N-(4-fluorophenyl)anthracene-9-sulfonamide (5b) and N-((1H-benzo[d]imidazol-2-yl)methyl)anthracene-9-sulfonamide (10) showed the significant selective cytotoxic effect over breast carcinoma cell lines (MCF-7). All the compounds are subjected to explore their safety on normal human skin cell lines (BJ-1), the results revealed that all the compounds are safe and have insignificant weak cytotoxicity over normal human cells.

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