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芳香化酶抑制剂的研究进展 被引量:7

Recent development in the studies on aromatase inhibitors
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摘要 芳香化酶是雌激素生物合成过程中的一个关键酶,抑制芳香化酶的活性就可以抑制雌激素的生成,从而减少绝经后妇女乳腺癌等疾病的发病率。以芳香化酶为靶标的研究一直都是抑制剂研究的热点,目前已有多个芳香化酶抑制剂进入临床试验阶段或已上市,该文对近年来芳香化酶抑制剂的研究进行综述。 Aromatase is the key enzyme in estrogen biosynthesis. Aromatase inhibitors, by means of inhibiting the process of estrogen biosynthesis, are proved to be effective in breast cancer and other diseases occured in postmenopausal women. Therefore, scientific research have been carried out on new aromatase inhibitors, some of which have been taken into clinical trials or market. Recent development of aromatase inhibitors were reviewed.
机构地区 吉林大学药学院
出处 《中国药物化学杂志》 CAS CSCD 2010年第1期70-76,共7页 Chinese Journal of Medicinal Chemistry
关键词 药物化学 雌激素 芳香化酶抑制剂 medicinal chemistry estrogen aromatase inhibitor
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  • 1KITAWAKI J, KADO N, ISHIHARA H, et al. Endometriosis: the pathophysiology as an estrogen-dependent disease [J]. J Steroid Biochem Mol Biol, 2003,83 ( 1/5 ) : 149 - 155.
  • 2KARKOLA S,HOELTJE H,WAHALA K. A three- dimensional model of CYP19 aromatase for structure-based drug design [ J ]. J Steroid Biochem Mol Biol,2007,105 ( 1/5) :63 - 70.
  • 3ZILEMBO N, BAJETTA E, NOBERASCO C, et al. Formestane: an effective first-line endocrine treatment for advanced breast cancer[J]. J Cancer Res Clin Oncol, 1995,121 (6) :378 - 382.
  • 4MLINERITSCH B, TAUSCH C, SINGER C, et al. Exemestane as primary systemic treatment for hormone receptor positive post-menopausal breast cancer patients:a phase II trial of the Austrian breast and colorectal cancer study group ( ABCSG-17 ) [ J ]. Breast Cancer Res Treat,2008,112 ( 1 ) :203 - 213.
  • 5NUMAZAWA M, YAMADA K, NITA S, et al.Role of hydrophilic interaction in binding of hydroxylated 3-deoxy C19 steroids to the active site of aromatase[ J ]. J Med Chem, 2001,44 ( 24 ) : 4277 - 4283.
  • 6MARGARIDA C, ELISIRIO S, GEORIGINA S, et al. Structure-activity relationships of new A, D-ring modified steroids as aromatase inhibitors: design, synthesis and biological activity evaluation [ J ]. J Med Chem ,2005 ,48 (20) : 6379 - 6385.
  • 7MARGARIDA C, ELISIRIO S, GEORIGINA S, et al. Synthesis and biochemical studies of 17-substitu- ted androst-3-enes and 3,4-epoxyandrostanes as aromatase inhibitors [ J ]. Steroids, 2008, 73 ( 14 ) : 1409 - 1415.
  • 8GOSS P. Pre-clinical and clinical review of vorozole, a new third generation aromatase inhibitor[ J ]. Breast Cancer Res Treat, 1998, 49 ( Suppl. 1 ) : 59 - 61.
  • 9TOMINAGA T, SUZUKI T. Early phase II study of the new aromatase inhibitor YM511 in postmenopausal patients with breast cancer. Difficulty in clinical dose recommendation based on preclinical and phase I findings [ J ]. Anticancer Res, 2003, 23 ( 4 ) : 3533 - 3542.
  • 10MAKELA T, WAHALA K, HASE T. Synthesis of enterolactone and enterodiol precursors as potential inhibitors of human estrogen synthetase(aromatase) [ J]. Steroids ,2000,65 ( 8 ) :437 - 441.

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