title: Synthesis and Evaluation of Estradiol Derivatives as Anti-Breast Cancer Agents.
abstract: 3-N-alkyloxyestradiol derivatives were synthesized, characterized and tested for activity in MCF-7 human breast cancer cells. Among the compounds, the diisopropyl and piperidinyl derivatives were found to be more active than 4-hydroxytamoxifen (HO-Tam), the active metabolite of tamoxifen based upon IC(50) values. The IC(50)s were correlated with structures using molecular modeling.
authors.affiliation: Florida A&M University College of Pharmacy and Pharmaceutical Sciences, Tallahassee, Florida 32307, USA; Tel: 1-850-599-3110; fax: 1-850-599-3323.
authors.forename: John S
authors.initials: JS
authors.lastname: Cooperwood
authors.forename: Jesse
authors.initials: J
authors.lastname: Edwards
authors.forename: Musiliyu
authors.initials: M
authors.lastname: Musa
authors.forename: Devora
authors.initials: D
authors.lastname: Simmons
authors.forename: Abdul D
authors.initials: AD
authors.lastname: Mian
authors.forename: Kwon-Kyun
authors.initials: KK
authors.lastname: Park
authors.forename: Zhongliang
authors.initials: Z
authors.lastname: Wan