Synthesis and identification of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs with dissociated antiprogesterone activities.
A series of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs have been evaluated for their antagonist hormonal properties using the T47D cell-based alkaline phosphatase assay and the A549 cell-based functional assay. Some of the compounds showed highly potent, and more selective antiprogestational activity against antiglucocorticoid activity than mifepristone (RU 486).
Jin
Chunyang
C
Center for Organic and Medicinal Chemistry, RTI International, PO Box 12194, Research Triangle Park, NC 27709, USA. cjin@rti.org
Manikumar
G
G
Kepler
John A
JA
Cook
C Edgar
CE
Allan
George F
GF
Kiddoe
Margaret
M
Bhattacharjee
Sheela
S
Linton
Olivia
O
Lundeen
Scott G
SG
Sui
Zhihua
Z
D002460:Cell Line; D006801:Humans; D010080:Oxazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D011374:Progesterone / Q000037:antagonists & inhibitors*
D010080:Oxazoles; D011374:Progesterone