Synthesis and Evaluation of Estradiol Derivatives as Anti-Breast Cancer Agents.
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.
Cooperwood
John S
JS
Florida A&M University College of Pharmacy and Pharmaceutical Sciences, Tallahassee, Florida 32307, USA; Tel: 1-850-599-3110; fax: 1-850-599-3323.
Edwards
Jesse
J
Musa
Musiliyu
M
Simmons
Devora
D
Mian
Abdul D
AD
Park
Kwon-Kyun
KK
Wan
Zhongliang
Z