Novel chromene-derived selective estrogen receptor modulators useful for alleviating hot flushes and vaginal dryness.
A novel SERM (selective estrogen receptor modulators), 1-(R), a chromene-derived bisbenzopyran, was discovered to alleviate hot flushes and effectively increase vaginal fluidity in rats. Moreover, 1-(R) was found to have beneficial effects on plasma cholesterol and bone metabolism while maintaining antiestrogenic activity in the uterus. The biological profile of its enantiomer 1-(S) was also evaluated.
Jain
Nareshkumar
N
Johnson & Johnson Pharmaceutical Research & Development LLC, 1000 Route 202, Raritan, New Jersey 08869, USA.
Kanojia
Ramesh M
RM
Xu
Jiayi
J
Jian-Zhong
Guo
G
Pacia
Emmanuel
E
Lai
Muh-Tsann
MT
Du
Fuyong
F
Musto
Amy
A
Allan
George
G
Hahn
DoWon
D
Lundeen
Scott
S
Sui
Zhihua
Z
D000818:Animals; D001578:Benzopyrans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001826:Body Fluids / Q000187:drug effects*; D015519:Bone Density / Q000187:drug effects; D002460:Cell Line; D002784:Cholesterol / Q000097:blood; D005260:Female; D019584:Hot Flashes / Q000188:drug therapy*; D006801:Humans; D009929:Organ Size / Q000187:drug effects; D010052:Ovariectomy; D051381:Rats; D020845:Selective Estrogen Receptor Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013237:Stereoisomerism; D014599:Uterus / Q000187:drug effects; D014621:Vagina / Q000187:drug effects* / Q000378:metabolism; D014623:Vaginal Diseases / Q000188:drug therapy*
D001578:Benzopyrans; D020845:Selective Estrogen Receptor Modulators; D002784:Cholesterol