Synthesis and antitumor activities of 3-modified 2-methoxyestradiol analogs.
The syntheses of 2-methoxyestradiol analogs with modifications at the 3-position are described. The analogs were assessed for their antiproliferative, antiangiogenic, and estrogenic activities. Several lead substituents were identified with similar or improved antitumor activities and reduced metabolic liability compared to 2-methoxyestradiol.
EntreMed, Inc., 9640 Medical Center Drive, Rockville, MD 20850, USA.
Lita S
LS
Suwandi
Gregory E
GE
Agoston
Jamshed H
JH
Shah
Arthur D
AD
Hanson
Xiaoguo H
XH
Zhan
Theresa M
TM
Lavallee
Anthony M
AM
Treston
D000077584:2-Methoxyestradiol; D000818:Animals; D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D004354:Drug Screening Assays, Antitumor; D004958:Estradiol / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D008297:Male; D051379:Mice; D008819:Mice, Nude; D008958:Models, Molecular; D008941:Spindle Apparatus / Q000187:drug effects*; D023041:Xenograft Model Antitumor Assays / Q000379:methods / Q000706:statistics & numerical data
D004958:Estradiol; D000077584:2-Methoxyestradiol