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N-Phenethyl and N-naphthylmethyl isatins and analogues as in vitro cytotoxic agents

Journal Article


Abstract


  • Arange of N-phenethyl,N-phenacyl, and N-(1- and 2-naphthylmethyl) derivatives of 5,7-dibromoisatin 2 were prepared byN-alkylation reactions. Their activity against human monocyte-like histiocytic lymphoma (U937), leukemia (Jurkat), and breast carcinoma (MDA-MB-231) cell lines was assessed. The results allowed further development of structureactivity relationships. The compound 5,7-dibromo-N-(1-naphthylmethyl)-1H-indole-2,3-dione 5a was the most potent against U937 cells with an IC50 value of 0.19 microM.

Publication Date


  • 2008

Citation


  • Matesic, L., Locke, J., Bremner, J. B., Pyne, S. G., Skropeta, D., Ranson, M. & Vine, K. L. (2008). N-Phenethyl and N-naphthylmethyl isatins and analogues as in vitro cytotoxic agents. Bioorganic and Medicinal Chemistry, 16 (6), 3118-3124.

Scopus Eid


  • 2-s2.0-40949155789

Ro Metadata Url


  • http://ro.uow.edu.au/scipapers/4059

Number Of Pages


  • 6

Start Page


  • 3118

End Page


  • 3124

Volume


  • 16

Issue


  • 6

Place Of Publication


  • http://www.elsevier.com/wps/find/journaldescription.cws_home/129/description#description

Abstract


  • Arange of N-phenethyl,N-phenacyl, and N-(1- and 2-naphthylmethyl) derivatives of 5,7-dibromoisatin 2 were prepared byN-alkylation reactions. Their activity against human monocyte-like histiocytic lymphoma (U937), leukemia (Jurkat), and breast carcinoma (MDA-MB-231) cell lines was assessed. The results allowed further development of structureactivity relationships. The compound 5,7-dibromo-N-(1-naphthylmethyl)-1H-indole-2,3-dione 5a was the most potent against U937 cells with an IC50 value of 0.19 microM.

Publication Date


  • 2008

Citation


  • Matesic, L., Locke, J., Bremner, J. B., Pyne, S. G., Skropeta, D., Ranson, M. & Vine, K. L. (2008). N-Phenethyl and N-naphthylmethyl isatins and analogues as in vitro cytotoxic agents. Bioorganic and Medicinal Chemistry, 16 (6), 3118-3124.

Scopus Eid


  • 2-s2.0-40949155789

Ro Metadata Url


  • http://ro.uow.edu.au/scipapers/4059

Number Of Pages


  • 6

Start Page


  • 3118

End Page


  • 3124

Volume


  • 16

Issue


  • 6

Place Of Publication


  • http://www.elsevier.com/wps/find/journaldescription.cws_home/129/description#description