title: Synthesis and evaluation of novel 4-amino-4,6-androstadiene-3,17-dione: an analog of formestane.
abstract: Synthesis of 4-amino-4,6-androstadiene-3,17-dione 7, an analog of formestane used in breast cancer therapy as an aromatase inhibitor, from 4-acetoxy-4-androstene-3,17-dione 2 is described. This is the first report of a 4-amino diene (4,6) system in this series of molecules. The new (7) and reported molecules were screened by the National Cancer Institute (NCI, Bethesda, USA) for in vitro antitumor activity against 60 human cancer cell lines. Molecule 7 showed best activity against breast cancer cell line (MCF-7).
authors.affiliation: Department of Oncology, University of Alberta, 11560 University Avenue, Edmonton, Alberta, Canada T6G 1Z2. sanjaysh@cancerboard.ab.ca
authors.forename: Sanjay K
authors.initials: SK
authors.lastname: Sharma
authors.forename: Weizhong
authors.initials: W
authors.lastname: Zheng
authors.forename: Alummoottil V
authors.initials: AV
authors.lastname: Joshua
authors.forename: Douglas N
authors.initials: DN
authors.lastname: Abrams
authors.forename: Alexander J B
authors.initials: AJ
authors.lastname: McEwan
mesh_terms: D000730:Androstadienes / Q000737:chemistry*; D000735:Androstenedione / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001141:Aromatase / Q000378:metabolism; D001943:Breast Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008956:Models, Chemical
chemical_list: D000730:Androstadienes; D000970:Antineoplastic Agents; D000735:Androstenedione; C038796:4,6-androstadiene-3,17-dione; D001141:Aromatase; C014594:formestane