Synthesis and structure-activity relationships of new non-steroidal progesterone receptor ligands.

作者: Ken-ichi Kurihara , Kiyoshi Tanabe , Yasuo Yamamoto , Rie Shinei , Keiichi Ajito

DOI: 10.1016/S0960-894X(99)00275-9

关键词: Methyl groupChemistryProgesterone receptorNon steroidalStereochemistryLactoneChemical synthesisIn vitro

摘要: Abstract In order to study structure-activity relationships, a series of new non-steroidal progesterone receptor ligands based on PF1092A 1) was synthesized with structural modifications (mostly introduction or removal methyl group) at the 3-, 4-, 5-, 7- 9-position in 6-acetoxy-4a, 5, 6, 7-tetrahydro-3, 4a, 5-trimethylnaphtho[2, 3 - b ]furan-2(4 H )-one 2) skeleton. Critical positions for high binding affinity were identified.

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