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

Authors

John B. Bremner, University of WollongongFollow
Stephen G. Pyne, University of WollongongFollow
Marie Ranson, University of WollongongFollow
Danielle Skropeta, University of WollongongFollow
Julie Locke, University of WollongongFollow
Lidia MatesicFollow
Kara L. Perrow, University of WollongongFollow

RIS ID

24416

Publication Details

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.

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.