Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain.
An optimized side chain for dihydrobenzoxathiin SERAMs was discovered and attached to four dihydrobenzoxathiin platforms. The novel SERAMs show exceptional estrogen antagonist activity in uterine tissue and an MCF-7 breast cancer cell assay.
Blizzard
Timothy A
TA
Merck Research Laboratories, RY800-B116, P.O. Box 2000, Rahway, NJ 07065, USA. tim.blizzard@merck.com
DiNinno
Frank
F
Chen
Helen Y
HY
Kim
Seongkon
S
Wu
Jane Y
JY
Chan
Wanda
W
Birzin
Elizabeth T
ET
Yang
Yi Tien
YT
Pai
Lee-Yuh
LY
Hayes
Edward C
EC
DaSilva
Carolyn A
CA
Rohrer
Susan P
SP
Schaeffer
James M
JM
Hammond
Milton L
ML
D000818:Animals; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D004965:Estrogen Antagonists / Q000138:chemical synthesis / Q000494:pharmacology; D005260:Female; D006801:Humans; D010075:Oxathiins / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011960:Receptors, Estrogen / Q000737:chemistry* / Q000378:metabolism; D020845:Selective Estrogen Receptor Modulators / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014599:Uterus / Q000187:drug effects / Q000254:growth & development
D004965:Estrogen Antagonists; D010075:Oxathiins; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators; C500019:dihydrobenzoxathiin