Synthesis and antimitotic activity of novel 2-methoxyestradiol analogs.
The syntheses and antimitotic activity of several novel 2-methoxyestradiol analogs are described. Structural modifications investigated include introduction of additional unsaturation in rings B and D; inversion at C-13; and substitution at the C-2, C-15, C-16, and C-7 alpha positions. Of 15 analogs synthesized, 2 have demonstrated superior biological activities compared to 2-methoxyestradiol.
Rao
Pemmaraju N
PN
Department of Organic Chemistry, Southwest Foundation for Biomedical Research, P O Box 760549, San Antonio, TX 78245-0549, USA. pnrao@icarus.sfbr.org
Cessac
James W
JW
Tinley
Tina L
TL
Mooberry
Susan L
SL
D000077584:2-Methoxyestradiol; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001011:Aorta; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D004958:Estradiol / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D008870:Microtubules / Q000187:drug effects; D008938:Mitosis / Q000187:drug effects; D015394:Molecular Structure; D009131:Muscle, Smooth, Vascular / Q000166:cytology / Q000187:drug effects; D051381:Rats; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D004958:Estradiol; D000077584:2-Methoxyestradiol