非甾体类孕酮受体配体构效关系的研究进展

The structure-activity relationship of nonsteroidal progesterone receptor ligands

孕酮受体配体(PRLs)通过孕酮受体介导发挥作用,有广泛的妇科疾病治疗前景。目前临床用药多为甾体类,不良反应多,临床应用极为有限。非甾体类PRLs具有高度的受体和组织选择性,有望降低不良反应,扩大其在临床上的应用。文中分类综述近年来非甾体类PRLs的研发进展,其中包括吲唑类、哒嗪类、苯并吡喃并喹啉类、苯并嗯嗪类、吲哚类、苯并咪唑和苯并噻唑类、氢化喹啉、吡唑类、二氮革类、苯并吲哚及萘并呋喃类化合物。

Progesterone receptor ligands （PRLs） function via progesterone receptor, and have potentially therapeutic applications in gynecological diseases. Because most clinically used drugs are steroidal derivatives and usually cause various adverse drug reactions, their applications are extremely limited. Nonsteroidal PRLs with high selectivity for receptors and tissues are expected to lower the adverse reactions, and to extend their uses in clinic. These PRLs developed in recent years are classified as indazoles, pyridazines, chrome-noquinolines, benzoxazines, indoles, benzimidazolones and benzothiazolones, quinolines, pyrazoles, diazepines, benzindolones, and naphtho- furanones.