非甾体孕酮受体配体（I）：新型四氢萘并呋喃酮衍生物的合成与构效关系
Nonsteroidal progesterone receptor ligands (I): synthesis and SAR of new tetrahydronaphthofuranone derivatives.
作者信息
Shinei Rie, Kurihara Ken-ichi, Tanabe Kiyoshi, Tabata Yuji, Kurata Yasushi, Hoshiko Shigeru, Okonogi Tsuneo
机构信息
Pharmaceutical Research Department, Meiji Seika Kaisha, Ltd., Yokohama 222-8567, Japan.
出版信息
Bioorg Med Chem. 2006 Jul 15;14(14):4850-61. doi: 10.1016/j.bmc.2006.03.018. Epub 2006 Mar 31.
We have synthesized a series of nonsteroidal progesterone receptor (PR) ligands, tetrahydronaphthofuranones, structurally based on the fungal metabolite PF1092C. Structure-activity relationship studies revealed that substituents at the 6- and 7-positions were critical for PR binding affinity and for agonist or antagonist activity. Compounds in this series, exemplified by 19i, exhibited high affinity and high specificity for PR over other steroid hormone receptors and acted as selective PR antagonists. Further modification of PF1092C may generate compounds of potential pharmacological interest.
我们基于真菌代谢产物PF1092C，合成了一系列非甾体类孕酮受体（PR）配体——四氢萘并呋喃酮。构效关系研究表明，6位和7位的取代基对于PR结合亲和力以及激动剂或拮抗剂活性至关重要。以19i为例，该系列化合物对PR表现出高于其他甾体激素受体的高亲和力和高特异性，并作为选择性PR拮抗剂发挥作用。对PF1092C的进一步修饰可能会产生具有潜在药理学意义的化合物。
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