title: N-phenethyl and N-naphthylmethyl isatins and analogues as in vitro cytotoxic agents.
abstract: A range of N-phenethyl, N-phenacyl, and N-(1- and 2-naphthylmethyl) derivatives of 5,7-dibromoisatin 2 were prepared by N-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 structure-activity relationships. The compound 5,7-dibromo-N-(1-naphthylmethyl)-1H-indole-2,3-dione 5a was the most potent against U937 cells with an IC(50) value of 0.19 microM.
authors.affiliation: School of Chemistry, University of Wollongong, Wollongong, NSW 2522, Australia. lm66@uow.edu.au
authors.forename: Lidia
authors.initials: L
authors.lastname: Matesic
authors.forename: Julie M
authors.initials: JM
authors.lastname: Locke
authors.forename: John B
authors.initials: JB
authors.lastname: Bremner
authors.forename: Stephen G
authors.initials: SG
authors.lastname: Pyne
authors.forename: Danielle
authors.initials: D
authors.lastname: Skropeta
authors.forename: Marie
authors.initials: M
authors.lastname: Ranson
authors.forename: Kara L
authors.initials: KL
authors.lastname: Vine
mesh_terms: D000478:Alkylation; D000970:Antineoplastic Agents / Q000737:chemistry*; D001943:Breast Neoplasms / Q000188:drug therapy; D045744:Cell Line, Tumor; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D007510:Isatin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D007938:Leukemia / Q000188:drug therapy; D008223:Lymphoma / Q000188:drug therapy; D008297:Male; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D007510:Isatin