甾体类芳香酶抑制剂的构效关系与研究进展
Structure activity relationship and the research progress of steroidal aromatase inhibitors
摘要
芳香酶是研究抗乳腺癌药物的新靶酶。本文从作用机制。
Aromatase is a new target enzyme for designing anti breast cancer drugs.The research progress of steroidal aromatase inhibitors in the mechanism and structure activity relationship were reviewed.
出处
《中国药物化学杂志》
CAS
CSCD
2002年第5期298-304,共7页
Chinese Journal of Medicinal Chemistry
关键词
甾体类芳香酶抑制剂
构效关系
研究进展
抗癌药
抗乳腺癌药物
aromatase
steroidal aromatase inhibitor
anti breast cancer drug
structure activity relationship
参考文献32
-
1Oh SS,Robinson CH.Mechanism of human placental aromatase:A new active site model[J].J Steroid Biochem Mole Biol,1993,44(4-6):389-397.
-
2Brueggemeier RW,Floyd EE,Counsell RE.Synthesis and biochemical evaluation of inhibitors of estrogen Biosynthesis[J].J Med Chem,1978,21(10):1007-1011.
-
3Numazawa M,Tachibana M.A-or B-ring-substitated derivatives of androst-4-ene-3,6,17-trione as aromatase inhibitors.Structure-activity relation-ships[J].Steroids,1994,59(10):579-585.
-
4Korzekwa KR,Trager WF,Smith SJ,et al.Theoretical studies on the mechanism of conversion of androgens to estrogens by aromatase[J].Biochem,1991,30(25):6155-6162.
-
5Nishino Y,Scheider MR,Michna H.Antitumor effect of specific aromatase inhibitor:1-methyl-androsta-1,4-diene-3,17-dione (atamestane),in female rats bearing DMBA-induced mammary tumors[J].J Steroid Biochem,1989,34(1-6):435-441.
-
6Miyairis S,Fishman J.3-Mthylene-substituted androgens as novel aromatization inhibitors.Evidence of a requirement for C-3 oxygen in C-19 hydroxylations[J].J Biol Chem,1986,261(15):6772-6777.
-
719-Oxygenation of C19-steroids with an A,B-ring enone structure competitive inhibitors of estrogen biosynthesis,with human placental aromatase[J].Bio Pharm Bull,2001,24(4):332-335.
-
8Wiseman LR,Mctavish D.Foremestane.a review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in the management of breast cancer and prostatic cancer[J].Drugs,1993,45(1):66-84.
-
9Di Salle E,Giudici D,Orati G.4-Aminoandrostenedione derivatives:a novel class of irreversible aromatase inhibitors.Comparision with FCF 24304 and 4-hydroxyandrostenedione[J].J Steroid Biochem Mol Biol,1990,37(3):369-372.
-
10Abul-Hajj,Yusaf J.Aromatase inhibition by 4-thiosubstituted-4-androstone-3,17-dione derivatives[J].J Steroid Biochem,1990,35(1-3):139-143.
-
1许关煜.企业[J].中国处方药,2013,11(1):22-22.
-
2韩伟,阎雪莹,丁文财,朱艳华.抗乳腺癌药物的研究现状[J].黑龙江医药,2014,27(5):1027-1029. 被引量:6
-
3张雅德.用抗乳腺癌药物治疗子宫内膜异位[J].国外医学情报,2000,21(10):29-29.
-
4抗乳腺癌药物他莫昔芬在精神病治疗领域的突破[J].中华医学信息导报,2007,22(19).
-
5王晔,项富海.芳香化酶抑制剂在乳腺癌治疗中的运用[J].国外医学(肿瘤学分册),2005,32(8):597-600. 被引量:2
-
6张姝,罗东林.抗乳腺癌药物福美司坦的研究进展[J].中国药房,2015,26(32):4606-4608. 被引量:2
-
7两基因变异致蒽环类抗乳腺癌药物失效[J].临床合理用药杂志,2010,3(4):49-49.
-
8陈本川,陈历胜.2009年世界最畅销的200种处方药(续二)[J].医药导报,2011,30(3).
-
9杨巍.抗乳腺癌药物对胃癌有效(曲妥珠单抗)[J].药品评价,2010,7(24):50-50.
-
10靳朝东,许瑞征,薛津.抗癌药A608中有机溶剂残留量的测定[J].现代仪器,2002,38(1):44-45.