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.
Merck Research Laboratories, RY800-B116, P.O. Box 2000, Rahway, NJ 07065, USA. tim.blizzard@merck.com
Timothy A
TA
Blizzard
Frank
F
DiNinno
Helen Y
HY
Chen
Seongkon
S
Kim
Jane Y
JY
Wu
Wanda
W
Chan
Elizabeth T
ET
Birzin
Yi Tien
YT
Yang
Lee-Yuh
LY
Pai
Edward C
EC
Hayes
Carolyn A
CA
DaSilva
Susan P
SP
Rohrer
James M
JM
Schaeffer
Milton L
ML
Hammond
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