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.
Suwandi
Lita S
LS
EntreMed, Inc., 9640 Medical Center Drive, Rockville, MD 20850, USA.
Agoston
Gregory E
GE
Shah
Jamshed H
JH
Hanson
Arthur D
AD
Zhan
Xiaoguo H
XH
Lavallee
Theresa M
TM
Treston
Anthony M
AM
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